Displaying publications 1 - 20 of 37 in total

Abstract:
Sort:
  1. Fulltext X-Linked Gusher Disease DFNX2 in Children, a Rare Inner Ear Dysplasia with Mixed Hearing and Vestibular Loss
    Dasgupta S, Hong J, Morris R, Iqbal J, Lennox-Bowley A, Saniasiaya J
    Audiol Res, 2023 Aug 04;13(4):600-614.
    PMID: 37622928 DOI: 10.3390/audiolres13040052
    Conductive hearing losses are typically present in disorders of the external/middle ear. However, there is a rare group of inner ear conditions called third windows that can also generate a conductive hearing loss. This is due to an abnormal connection between the middle and the inner ear or between the inner ear and the cranial cavity. X-linked gusher disorder is an extremely rare congenital inner ear dysplastic syndrome with an abnormal connection due to a characteristic incomplete cochlear partition type III and an incomplete internal auditory meatus fundus. The disorder is inherited in an X-linked fashion due to the mutation of the POU3F4 gene. We present two siblings diagnosed with the condition and their long-term follow-ups. They both presented audiovestibular symptoms and showed progressive mixed losses and bilateral vestibular weakness. They were treated with cochlear implant, digital amplification and with vestibular rehabilitation. Significant others around them were involved in their journey with the medical team, and in both, a very favourable outcome was achieved. This is the first time that we have reported evolving audiovestibular function with vestibular quantification in X-linked gusher disorder and emphasize on the multidisciplinary holistic approach to manage these children effectively.
  2. Exploring chromone sulfonamides and sulfonylhydrazones as highly selective ectonucleotidase inhibitors: Synthesis, biological evaluation and in silico study
    Younus HA, Saeed M, Mahmood A, Jadoon MSK, Hameed A, Asari A, et al.
    Bioorg Chem, 2023 May;134:106450.
    PMID: 36924652 DOI: 10.1016/j.bioorg.2023.106450
    Ectonucleotidases, a well-known superfamily of plasma membrane located metalloenzymes plays a central role in mediating the process of purinergic cell signaling. Major functions performed by these enzymes include the hydrolysis of extracellular nucleosides and nucleotides which are considered as important cell-signaling molecules. Any (patho)-physiologically induced disruption in this purinergic cell signaling leads to several disorders, hence these enzymes are important drug targets for therapeutic purposes. Among the major challenges faced in the design of inhibitors of ectonucleotidases, an important one is the lack of selective inhibitors. Access to highly selective inhibitors via a facile synthetic route will not only be beneficial therapeutically, but will also lead to an increase in our understanding of intricate interplay between members of ectonucleotidase enzymes in relation to their selective activation and/or inhibition in different cells and tissues. Herein we describe synthesis of highly selective inhibitors of human intestinal alkaline phosphatase (h-IAP) and human tissue non-specific alkaline phosphatase (h-TNAP), containing chromone sulfonamide and sulfonylhydrazone scaffolds. Compound 1c exhibited highest (and most selective) h-IAP inhibition activity (h-IAP IC50 = 0.51 ± 0.20 µM; h-TNAP = 36.5%) and compound 3k showed highest activity and selective inhibition against h-TNAP (h-TNAP IC50 = 1.41 ± 0.10 µM; h-IAP = 43.1%). These compounds were also evaluated against another member of ectonucleotidase family, that is rat and human ecto-5'-nucleotidase (r-e5'NT and h-e5'NT). Some of the compounds exhibited excellent inhibitory activity against ecto-5'-nucleotidase. Compound 2 g exhibited highest inhibition against h-e5'NT (IC50 = 0.18 ± 0.02 µM). To rationalize the interactions with the binding site, molecular docking studies were carried out.
  3. Performance evaluation of phosphonium based deep eutectic solvents coated cerium oxide nanoparticles for CO2 capture
    Ahmad T, Iqbal J, Bustam MA, Babar M, Tahir MB, Sagir M, et al.
    Environ Res, 2023 Apr 01;222:115314.
    PMID: 36738770 DOI: 10.1016/j.envres.2023.115314
    The critical challenge being faced by our current modern society on a global scale is to reduce the surging effects of climate change and global warming, being caused by anthropogenic emissions of CO2 in the environment. Present study reports the surface driven adsorption potential of deep eutectic solvents (DESs) surface functionalized cerium oxide nanoparticles (CeNPs) for low pressure CO2 separation. The phosphonium based DESs were prepared using tetra butyl phosphoniumbromide as hydrogen bond acceptor (HBA) and 6 acids as hydrogen bond donors (HBDs). The as-developed DESs were characterized and employed for the surface functionalization of CeNPs with their subsequent utilization in adsorption-based CO2 adsorption. The synthesis of as-prepared DESs was confirmed through FTIR measurements and absence of precipitates, revealed through visual observations. It was found that DES6 surface functionalized CeNPs demonstrated 27% higher adsorption performance for CO2 capturing. On the contrary, DES3 coated CeNPs exhibited the least adsorption progress for CO2 separation. The higher adsorption performance associated with DES6 coated CeNPs was due to enhanced surface affinity with CO2 molecules that must have facilitated the mass transport characteristics and resulted an enhancement in CO2 adsorption performance. Carboxylic groups could have generated an electric field inside the pores to attract more polarizable adsorbates including CO2, are responsible for the relatively high values of CO2 adsorption. The quadruple movement of the CO2 molecules with the electron-deficient and pluralizable nature led to the enhancement of the interactive forces between the CO2 molecules and the CeNPs decorated with the carboxylic group hydrogen bond donor rich DES. The current findings may disclose the new research horizons and theoretical guidance for reduction in the environmental effects associated with uncontrolled CO2 emission via employing DES surface coated potential CeNPs.
  4. Fulltext Poly (Vinyl Alcohol)/Agar Hydrogel Electrolytes Based Flexible All-in-One Supercapacitors with Conducting Polyaniline/Polypyrrole Electrodes
    Hasan K, Bashir S, Subramaniam R, Kasi R, Kamran K, Iqbal J, et al.
    Polymers (Basel), 2022 Nov 07;14(21).
    PMID: 36365772 DOI: 10.3390/polym14214784
    The major components of supercapacitor are electrodes and electrolytes which are fabricated using various materials and methods. Hydrogel is one such material that is used in supercapacitors as electrodes and electrolytes or both. Hydrogels are usually described as a soft and porous network of polymer materials that can swell in water because of the hydrophilic nature of its polymer chains, compriseng a 3D structure. It is well known that supercapacitors possess high-power density but low energy density. For enhancing energy density of these electrochemical cells and a boost in its electrochemical performance and specific capacity, binder free conducting polymer hydrogel electrodes have gained immense attention, especially polyaniline (PANI) and polypyrrole (PPy). Therefore, in this work, chemically crosslinked PVA/Agar hydrogel electrolytes have been prepared and employed. Agar has been added in PVA since it is environmentally friendly, biodegradable, and cost-effective natural polymer. Subsequently, the binder free polyaniline/polypyrrole electrodes were grown on the PVA/Agar hydrogel electrolytes to fabricate all-in-one flexible hydrogels. The synthesized hydrogels were characterized using X-ray diffraction (XRD) analysis, Fourier transform infrared (FTIR) analysis, Field emission scanning electron microscope (FESEM) and mechanical studies. Then, the all-in-one flexible supercapacitors were fabricated using the hydrogels. The electrochemical studies such cyclic voltammetry (CV), galvanic charge discharge (GCD), and electrochemical impedance spectroscopy (EIS) studies. The fabricated all-in-one lamination free supercapacitors showed promising results and by comparing all four samples, PAP2 where 5 mL of PVA was used in combination with 3 mL of Agar and 5 mL of PANI and PPy each, exhibited the highest areal capacitance of 750.13 mF/cm2, energy density of 103.02 μWh/cm2, and 497.22 μW/cm2 power density. The cyclic stability study revealed the 149% capacity retention after 15,000 cycles.
  5. Fulltext A Novel Design and Development of a Strip-Fed Circularly Polarized Rectangular Dielectric Resonator Antenna for 5G NR Sub-6 GHz Band Applications
    Illahi U, Iqbal J, Irfan M, Ismail Sulaiman M, Khan MA, Rauf A, et al.
    Sensors (Basel), 2022 Jul 25;22(15).
    PMID: 35898037 DOI: 10.3390/s22155531
    In this article, a rectangular dielectric resonator antenna (RDRA) with circularly polarized (CP) response is presented for 5G NR (New Radio) Sub-6 GHz band applications. A uniquely shaped conformal metal feeding strip is proposed to excite the RDRA in higher-order mode for high gain utilization. By using the proposed feeding mechanism, the degenerate mode pair of the first higher-order, i.e., TEδ13x at 4.13 GHz and TE1δ3y, at 4.52 GHz is excited to achieve a circularly polarized response. A circular polarization over a bandwidth of ~10%, in conjunction with a wide impedance matching over a bandwidth of ~17%, were attained by the antenna. The CP antenna proposed offers a useful gain of ~6.2 dBic. The achieved CP bandwidth of the RDRA is good enough to cover the targeted 5G NR bands around 4.4−4.8 GHz, such as n79. The proposed antenna configuration is modelled and optimized using computer simulation technology (CST). A prototype was built to confirm (validate) the performance estimated through simulation. A good agreement was observed between simulated and measured results.
  6. Deep eutectic solvent mediated synthesis of 3,4-dihydropyrimidin-2(1H)-ones and evaluation of biological activities targeting neurodegenerative disorders
    Saleem Khan M, Asif Nawaz M, Jalil S, Rashid F, Hameed A, Asari A, et al.
    Bioorg Chem, 2022 01;118:105457.
    PMID: 34798458 DOI: 10.1016/j.bioorg.2021.105457
    Substitution of hazardous and often harmful organic solvents with "green" and "sustainable" alternative reaction media is always desirous. Ionic liquids (IL) have emerged as valuable and versatile liquids that can replace most organic solvents in a variety of syntheses. However, recently new types of low melting mixtures termed as Deep Eutectic Solvents (DES) have been utilized in organic syntheses. DES are non-volatile in nature, have sufficient thermal stability, and also have the ability to be recycled and reused. Hence DES have been used as alternative reaction media to perform different organic reactions. The availability of green, inexpensive and easy to handle alternative solvents for organic synthesis is still scarce, hence our interest in DES mediated syntheses. Herein we have investigated Biginelli reaction in different DES for the synthesis of 3,4-dihydropyrimidin-2(1H)-ones. Monoamine oxidases and cholinesterases are important drug targets for the treatment of various neurological disorders such as Alzheimer's disease, Parkinson's disease, depression and anxiety. The compounds synthesized herein were evaluated for their inhibitory potential against these enzymes. Some of the compounds were found to be highly potent and selective inhibitors. Compounds 1 h and 1c were the most active monoamine oxidase A (MAO A) (IC50 = 0.31 ± 0.11 µM) and monoamine oxidase B (MAO B) (IC50 = 0.34 ± 0.04 µM) inhibitors respectively. All compounds were selective AChE inhibitors and did not inhibit BChE (<29% inhibition). Compound 1 k (IC50 = 0.13 ± 0.09 µM) was the most active AChE inhibitor.
  7. Fulltext Physio-chemical characterization of indigenous agricultural waste materials for the development of potting media
    Kiran S, Iqbal J, Danish S, Bakhsh A, Bukhari SIUS, Bibi F, et al.
    Saudi J Biol Sci, 2021 Dec;28(12):7491-7498.
    PMID: 34867054 DOI: 10.1016/j.sjbs.2021.08.058
    Organic residues are an important factor that directly affects fruiting tree seedlings' health at earlier stages. It provides a suitable environment for seedling growth by providing better nutrient ions, water, and aeration. However, low organic contents and high shrinkage of most organic materials mostly deteriorate ideal potting media characteristics. Low aeration, high water, and nutrients leaching decrease seedling growth and cause a significant loss of valuable resources. That is why the current study was conducted to screen out the best indigenous materials based on particle size to produce good characteristics bearing potting media. For that, eight different ingredients, i.e., "sugarcane", "coconut coir", "wheat straw", "rice straw", "corn cob", "leaf litter", "farmyard manure", and "sunflower heads" were collected. Initially, all the materials were air-dried and processes as per requirement. After grinding, three particles size (fine = < 2 mm, medium = 3 mm and coarse = 5 mm) were separated by sieving. Results showed that decreasing particle size in "rice straw", "corn cob", "farmyard manure," and "sunflower head" decreased leachate pH. Higher EC in leachates was negatively correlated with particle size in all potting media ingredients. Except for farmyard manure, fine particle size increases the water-holding ability of potting media ingredients. However, air-filled porosity was associated with a decrease in particle size of potting media in gradients. In conclusion, farmyard manure, "sunflower heads", "leaf litter" and "sugarcane" should be incorporated while making a combination for potting media. More investigations are suggested by mixing different particle size ingredients to prepare potting media.
  8. Fabrication and dialysis performance of functionalized multiwall carbon nanotubes integrated cellulose acetate/poly(vinylpyrrolidone) membranes
    Ashraf MA, Islam A, Butt MA, Hussain T, Khan RU, Bashir S, et al.
    Int J Biol Macromol, 2021 Nov 30;191:872-880.
    PMID: 34571131 DOI: 10.1016/j.ijbiomac.2021.09.131
    Mixed matrix membranes (MMMs) of cellulose acetate/poly(vinylpyrrolidone) (CA/PVP) infused with acid functionalized multiwall carbon nanotubes (f-MWCNTs) were fabricated by an immersion phase separation technique for hemodialysis application. Membranes were characterized using FTIR, water uptake, contact angle, TGA, DMA and SEM analysis. The FTIR was used to confirm the bonding interaction between CA/PVP membrane matrix and f-MWCNTs. Upon addition of f-MWCNTs, TGA thermograms and glass transition temperature indicated improved thermal stability of MMMs. The surface morphological analysis demonstrated revealed uniform distribution of f-MWCNTs and asymmetric membrane structure. The water uptake and contact angle confirmed that hydrophilicity was increased after incorporation of f-MWCNTs. The membranes demonstrated enhancement in water permeate flux, bovine serum albumin (BSA) rejection with the infusion of f-MWCNTs; whereas BSA based anti-fouling analysis using flux recovery ratio test shown up to 8.4% improvement. The urea and creatinine clearance performance of MMMs were evaluated by dialysis experiment. It has been found that f-MWCNTs integrated membranes demonstrated the higher urea and creatinine clearance with increase of 12.6% and 10.5% in comparison to the neat CA/PVP membrane. Thus, the prepared CA/PVP membranes embedded with f-MWCNTs can be employed for wide range of dialysis applications.
  9. Semicarbazones, thiosemicarbazone, thiazole and oxazole analogues as monoamine oxidase inhibitors: Synthesis, characterization, biological evaluation, molecular docking, and kinetic studies
    Qazi SU, Naz A, Hameed A, Osra FA, Jalil S, Iqbal J, et al.
    Bioorg Chem, 2021 10;115:105209.
    PMID: 34364054 DOI: 10.1016/j.bioorg.2021.105209
    A series of semicarbazone, thiosemicarbazone, thiazole, and oxazole derivatives were designed, synthesized, and examined for monoamine oxidase inhibition using two isoforms, i.e., MAO-A and MAO-B. Among all the analogues, 3c and 3j possessed substantial activity against MAO-A with IC50 values of 5.619 ± 1.04 µM and 0.5781 ± 0.1674 µM, respectively. Whereas 3d and 3j were active against monoamine oxidase B with the IC50 values of 9.952 ± 1.831 µM and 3.5 ± 0.7 µM, respectively. Other derivatives active against MAO-B were 3c and 3g with the IC50 values of 17.67 ± 5.6 µM and 37.18 ± 2.485 µM. Moreover, molecular docking studies were achieved for the most potent compound (3j) contrary to human MAO-A and MAO-B. Kinetic studies were also performed for the most potent analogue to evaluate its mode of interaction with MAO-A and MAO-B.
  10. Synthesis of indole-substituted thiosemicarbazones as an aldose reductase inhibitor: an in vitro, selectivity and in silico study
    Shehzad MT, Khan A, Halim SA, Hameed A, Imran A, Iqbal J, et al.
    Future Med Chem, 2021 07;13(14):1185-1201.
    PMID: 34148377 DOI: 10.4155/fmc-2020-0060
    Aim: Indole is an important component of many drug molecules, and its conjugation with thiosemicarbazone moiety would be advantageous in finding lead compounds for the development of diabetic complications. Methodology: We have designed, synthesized and evaluated a series of 17 indole-thiosemicarbazones (3a-q) as aldose reductase (ALR2) and aldehyde reductase (ALR1) inhibitors. Results: After in vitro evaluation, all indole-thiosemicarbazones showed significant inhibition against both enzyme ALR1 and ALR2 with IC50 in range of 0.42-20.7 and 1.02-19.1 μM, respectively. The docking study was also carried out to consider the putative binding of molecules with the target enzymes. Conclusion: Compound 3f was found to be most active and selective for ALR2. The indole-thiosemicarbazones series described here has selective hits for diabetes-mellitus-associated complications.
  11. Antimicrobial properties of multifunctional polypyrrole-cobalt oxide-silver nanocomposite against pathogenic bacteria and parasite
    Masri A, Abdelnasir S, Anwar A, Iqbal J, Numan A, Jagadish P, et al.
    Appl Microbiol Biotechnol, 2021 Apr;105(8):3315-3325.
    PMID: 33797573 DOI: 10.1007/s00253-021-11221-1
    BACKGROUND: Conducting polymer based nanocomposites are known to be effective against pathogens. Herein, we report the antimicrobial properties of multifunctional polypyrrole-cobalt oxide-silver nanocomposite (PPy-Co3O4-AgNPs) for the first time. Antibacterial activities were tested against multi-drug-resistant Gram-negative Escherichia coli (E. coli) and Gram-positive methicillin-resistant Staphylococcus aureus (MRSA) bacteria, while antiamoebic effects were assessed against opportunistic protist Acanthamoeba castellanii (A. castellanii).

    RESULTS: The ternary nanocomposite containing conducting polymer polypyrrole, cobalt oxide, and silver nanoparticles showed potent antimicrobial effects against these pathogens. The antibacterial assay showed that PPy-Co3O4-AgNPs exhibited significant bactericidal activity against neuropathogenic E. coli K1 at only 8 μg/mL as compared to individual components of the nanocomposite, whereas a 70 % inhibition of A. castellanii viability was observed at 50 μg/mL. Moreover, PPy-Co3O4-AgNPs were found to have minimal cytotoxicity against human keratinocytes HaCaT cells in vitro even at higher concentration (50 μg/mL), and also reduced the microbes-mediated cytopathogenicity against host cells.

    CONCLUSION: These results demonstrate that PPy-Co3O4-AgNPs hold promise in the development of novel antimicrobial nanomaterials for biomedical applications.

    KEY POINTS: •Synthesis of polypyrrole-cobalt oxide-silver (PPy-Co3O4-AgNPs) nanocomposite. •Antimicrobial activity of nanocomposite. •PPy-Co3O4-AgNPs hold promise for biomedical applications.

  12. Fulltext Hydrothermally Assisted Synthesis of Porous Polyaniline@Carbon Nanotubes-Manganese Dioxide Ternary Composite for Potential Application in Supercapattery
    Iqbal J, Ansari MO, Numan A, Wageh S, Al-Ghamdi A, Alam MG, et al.
    Polymers (Basel), 2020 Dec 05;12(12).
    PMID: 33291451 DOI: 10.3390/polym12122918
    In this study, ternary composites of polyaniline (PANI) with manganese dioxide (MnO2) nanorods and carbon nanotubes (CNTs) were prepared by employing a hydrothermal methodology and in-situ oxidative polymerization of aniline. The morphological analysis by scanning electron microscopy showed that the MnO2 possessed nanorod like structures in its pristine form, while in the ternary PANI@CNT/MnO2 composite, coating of PANI over CNT/MnO2, rods/tubes were evidently seen. The structural analysis by X-ray diffraction and X-ray photoelectron spectroscopy showed peaks corresponding to MnO2, PANI and CNT, which suggested efficacy of the synthesis methodology. The electrochemical performance in contrast to individual components revealed the enhanced performance of PANI@CNT/MnO2 composite due to the synergistic/additional effect of PANI, CNT and MnO2 compared to pure MnO2, PANI and PANI@CNT. The PANI@CNT/MnO2 ternary composite exhibited an excellent specific capacity of 143.26 C g-1 at a scan rate of 3 mV s-1. The cyclic stability of the supercapattery (PANI@CNT/MnO2/activated carbon)-consisting of a battery type electrode-demonstrated a gradual increase in specific capacity with continuous charge-discharge over ~1000 cycles and showed a cyclic stability of 119% compared to its initial value after 3500 cycles.
  13. Fulltext Cobalt Oxide Nanograins and Silver Nanoparticles Decorated Fibrous Polyaniline Nanocomposite as Battery-Type Electrode for High Performance Supercapattery
    Iqbal J, Numan A, Omaish Ansari M, Jafer R, Jagadish PR, Bashir S, et al.
    Polymers (Basel), 2020 Nov 27;12(12).
    PMID: 33261072 DOI: 10.3390/polym12122816
    In this study, silver (Ag) and cobalt oxide (Co3O4) decorated polyaniline (PANI) fibers were prepared by the combination of in-situ aniline oxidative polymerization and the hydrothermal methodology. The morphology of the prepared Ag/Co3O4@PANI ternary nanocomposite was studied by scanning electron microscopy and transmission electron microscopy, while the structural studies were carried out by X-ray diffraction and X-ray photoelectron spectroscopy. The morphological characterization revealed fibrous shaped PANI, coated with Ag and Co3O4 nanograins, while the structural studies revealed high purity, good crystallinity, and slight interactions among the constituents of the Ag/Co3O4@PANI ternary nanocomposite. The electrochemical performance studies revealed the enhanced performance of the Ag/Co3O4@PANI nanocomposite due to the synergistic/additional effect of Ag, Co3O4 and PANI compared to pure PANI and Co3O4@PANI. The addition of the Ag and Co3O4 provided an extended site for faradaic reactions leading to the high specific capacity. The Ag/Co3O4@PANI ternary nanocomposite exhibited an excellent specific capacity of 262.62 C g-1 at a scan rate of 3 mV s-1. The maximum energy and power density were found to be 14.01 Wh kg-1 and 165.00 W kg-1, respectively. The cyclic stability of supercapattery (Ag/Co3O4@PANI//activated carbon) consisting of a battery type electrode demonstrated a gradual increase in specific capacity with a continuous charge-discharge cycle until ~1000 cycles, then remained stable until 2500 cycles and later started decreasing, thereby showing the cyclic stability of 121.03% of its initial value after 3500 cycles.
  14. Fulltext Fundamental Concepts of Hydrogels: Synthesis, Properties, and Their Applications
    Bashir S, Hina M, Iqbal J, Rajpar AH, Mujtaba MA, Alghamdi NA, et al.
    Polymers (Basel), 2020 Nov 16;12(11).
    PMID: 33207715 DOI: 10.3390/polym12112702
    In the present review, we focused on the fundamental concepts of hydrogels-classification, the polymers involved, synthesis methods, types of hydrogels, properties, and applications of the hydrogel. Hydrogels can be synthesized from natural polymers, synthetic polymers, polymerizable synthetic monomers, and a combination of natural and synthetic polymers. Synthesis of hydrogels involves physical, chemical, and hybrid bonding. The bonding is formed via different routes, such as solution casting, solution mixing, bulk polymerization, free radical mechanism, radiation method, and interpenetrating network formation. The synthesized hydrogels have significant properties, such as mechanical strength, biocompatibility, biodegradability, swellability, and stimuli sensitivity. These properties are substantial for electrochemical and biomedical applications. Furthermore, this review emphasizes flexible and self-healable hydrogels as electrolytes for energy storage and energy conversion applications. Insufficient adhesiveness (less interfacial interaction) between electrodes and electrolytes and mechanical strength pose serious challenges, such as delamination of the supercapacitors, batteries, and solar cells. Owing to smart and aqueous hydrogels, robust mechanical strength, adhesiveness, stretchability, strain sensitivity, and self-healability are the critical factors that can identify the reliability and robustness of the energy storage and conversion devices. These devices are highly efficient and convenient for smart, light-weight, foldable electronics and modern pollution-free transportation in the current decade.
  15. Indole acrylonitriles as potential anti-hyperglycemic agents: Synthesis, α-glucosidase inhibitory activity and molecular docking studies
    Solangi M, Kanwal, Mohammed Khan K, Saleem F, Hameed S, Iqbal J, et al.
    Bioorg Med Chem, 2020 Nov 01;28(21):115605.
    PMID: 33065441 DOI: 10.1016/j.bmc.2020.115605
    One of the most prevailing metabolic disorder diabetes mellitus has become the global health issue that has to be addressed and cured. Different marketed drugs have been made available for the treatment of diabetes but there is still a need of introducing new therapeutic agents that are economical and have lesser or no side effects. The current study deals with the synthesis of indole acrylonitriles (3-23) and the evaluation of these compounds for their potential for α-glucosidase inhibition. The structures of these synthetic molecules were deduced by using different spectroscopic techniques. Acarbose (IC50 = 2.91 ± 0.02 μM) was used as standard in this study and the synthetic molecules (3-23) have shown promising α-glucosidase inhibitory activity. Compounds 4, 8, 10, 11, 14, 18, and 21 displayed superior inhibition of α-glucosidase enzyme in the range of (IC50 = 0.53 ± 0.01-1.36 ± 0.04 μM) as compared to the standard acarbose. Compound 10 (IC50 = 0.53 ± 0.01 μM) was the most effective inhibitor of this library and displayed many folds enhanced activity in contrast to the standard. Molecular docking of synthetic compounds was performed to verify the binding interactions of ligand with the active site of enzyme. This study had identified a number of potential α-glucosidase inhibitors that can be used for further research to identify a potent therapeutic agent against diabetes.
  16. Sulfonylhydrazones: Design, synthesis and investigation of ectonucleotidase (ALP & e5'NT) inhibition activities
    Younus HA, Hameed A, Mahmood A, Khan MS, Saeed M, Batool F, et al.
    Bioorg Chem, 2020 07;100:103827.
    PMID: 32402802 DOI: 10.1016/j.bioorg.2020.103827
    Medicinal importance of the sulfonylhydrazones is well-evident owing to their binding ability with zinc containing metalloenzymes. In the present study, we have synthesized different series of sulfonylhydrazones by using facile synthetic methods in good to excellent yield. All the successfully prepared sulfonylhydrazones were screened for ectonucleotidase (ALP & e5'NT) inhibitory activity. Among the chromen-2-one scaffold based sulfonylhydrazones, the compounds 7 was found to be most potent inhibitor for h-TNAP (human tissue non-specific alkaline phosphatase) and h-IAP (human intestinal alkaline phosphatase) with IC50 values of 1.02 ± 0.13 and 0.32 ± 0.0 3 µM respectively, compared with levamisole (IC50 = 25.2 ± 1.90 µM for h-TNAP) and l-phenylalanine (IC50 = 100 ± 3.00 µM for h-IAP) as standards. Further, the chromen-2-one based molecule 5a showed excellent activity against h-ecto 5'-NT (human ecto-5'-nucleotidase) with IC50 value of 0.29 ± 0.004 µM compared to standard, sulfamic acid (IC50 = 42.1 ± 7.8 µM). However, among the series of phenyl ring based sulfonylhydrazones, compound 9d was found to be most potent against h-TNAP and h-IAP with IC50 values of 0.85 ± 0.08 and 0.52 ± 0.03 µM, respectively. Moreover, in silico studies were also carried to demonstrate their putative binding with the target enzymes. The potent compounds 5a, 7, and 9d against different ectonucleotidases (h-ecto 5'-NT, h-TNAP, h-IAP) could potentially serve as lead for the development of new therapeutic agents.
  17. BSA Binding, molecular docking and in vitro biological screening of some new 1, 2, 4-triazole heterocycles bearing azinane nucleus
    Iqbal J, Rehman A, Abbasi MA, Siddiqui SZ, Khalid H, Laulloo SJ, et al.
    Pak J Pharm Sci, 2020 Jan;33(1):149-160.
    PMID: 32122843
    A series of new compounds (5a-q), derived from 5-(1-(4-nitrophenylsulfonyl) piperidin-4-yl)-4-phenyl-4H-1,2,4-triazole-3-thiol (3) were proficiently synthesized to evaluate their biological activities. 1-(4-Nitrophenylsulfonyl) piperidine-4-carbohydrazide (2) was refluxed with phenylisothiocyanate to yield an adduct which was cyclized to compound 3 by reflux reaction with 10 % potassium hydroxide. The targeted compounds 5a-q, were synthesized by stirring alkyl/aralkyl halides (4a-q) and compound 3 in a polar aprotic solvent. 1H-NMR, 13C-NMR, EI-MS and IR spectral techniques were employed to confirm the structures of all the synthesized compounds. The compounds were biologically evaluated for BSA binding studies followed by anti-bacterial, anti-inflammatory and acetylcholinesterase (AChE) activities. The active sites responsible for the best AChE inhibition were identified through molecular docking studies. Compound 5e bearing 4-chlorobenzyl moiety found most active antibacterial and anti-inflammatory agent among the synthesized compounds. The whole library of synthesized compounds except compounds 5d and 5f was found highly active for AChE inhibition and recommended for in vivo studies so that their therapeutic applications may come in utilization.
  18. Fulltext Requirements engineering issues causing software development outsourcing failure
    Iqbal J, Ahmad RB, Khan M, Fazal-E-Amin, Alyahya S, Nizam Nasir MH, et al.
    PLoS One, 2020;15(4):e0229785.
    PMID: 32271783 DOI: 10.1371/journal.pone.0229785
    Software development outsourcing is becoming more and more famous because of the advantages like cost abatement, process enhancement, and coping with the scarcity of needed resources. Studies confirm that unfortunately a large proportion of the software development outsourcing projects fails to realize anticipated benefits. Investigations into the failures of such projects divulge that in several cases software development outsourcing projects are failed because of the issues that are associated with requirements engineering process. The objective of this study is the identification and the ranking of the commonly occurring issues of the requirements engineering process in the case of software development outsourcing. For this purpose, contemporary literature has been assessed rigorously, issues faced by practitioners have been identified and three questionnaire surveys have been organized by involving experienced software development outsourcing practitioners. The Delphi technique, cut-off value method and 50% rule have also been employed. The study explores 150 issues (129 issues from literature and 21 from industry) of requirements engineering process for software development outsourcing, groups the 150 issues into 7 identified categories and then extricates 43 customarily or commonly arising issues from the 150 issues. Founded on 'frequency of occurrence' the 43 customarily arising issues have been ranked with respect to respective categories (category-wise ranking) and with respect to all the categories (overall ranking). Categories of the customarily arising issues have also been ranked. The issues' identification and ranking contribute to design proactive software project management plan for dealing with software development outsourcing failures and attaining conjectured benefits of the software development outsourcing.
  19. Fulltext Innovation in Chinese internet companies: A meta-frontier analysis
    Hafeez S, Arshad NI, Rahim LBAB, Shabbir MF, Iqbal J
    PLoS One, 2020;15(5):e0233278.
    PMID: 32437383 DOI: 10.1371/journal.pone.0233278
    The innovation of a particular company benefits the whole industry when innovation technology transfers to others. Similarly, the development and innovation in internet companies influence the development and innovation of the industry. This investigation has applied a unique approach of meta-frontier analysis to estimate and analyze the innovation in internet companies in China. A unique dataset of Chinese internet companies from 2000 to 2017 has been utilized to estimate and compare the innovation over the period of study. The change in technology gap ratio (TGR) and a shift in production function have translated into innovation which was overlooked by previous studies. It is found that the production function of internet companies is moving upward in the presence of external factors such as smartphones invention, mobile internet, mobile payments, and artificial intelligence, etc. Consequently, a sudden increase in TGR is captured due to the innovation of some companies. Hence, the average TE of the industry falls caused by the increased distance of other companies form industry production function. However, the innovation advantage defused when other companies start imitating and the average TE elevates. A steady increase in the TGR index revealed that the continuous innovation-based growth of some companies lifting the production frontier upward. This provides the opportunity for other companies to imitate and provides continuous growth in the industry. This study provides a novel methodological approach to measure innovation and also provide practical implication by empirical estimation of innovation in Chinese internet companies.
  20. Ultrasonication-assisted synthesis of novel strontium based mixed phase structures for supercapattery devices
    Iqbal MZ, Khan A, Numan A, Haider SS, Iqbal J
    Ultrason Sonochem, 2019 Dec;59:104736.
    PMID: 31473424 DOI: 10.1016/j.ultsonch.2019.104736
    An upsurge in sustainable energy demands has ultimately made supercapattery one of the important choice for energy storage, owing to highly advantageous energy density and long life span. In this work, novel strontium based mixed phased nanostructures were synthesized by using probe sonicator with sonication power 500 W at frequency of 20 kHz. The synthesized material was subsequently calcined at different temperature ranging from 200 to 800 °C. Structural and morphological analysis of the synthesized materials reveals the formation of mixed particle and rod like nanostructures with multiple crystal phases of strontium oxides and carbonates. Crystallinity, grain size and morphology of grown nanomaterials significantly improved with the increase of calcination temperature due to sufficient particle growth and low agglomeration. The electrochemical performance analysis confirms the redox activeness of the Sr-based electrode materials. Material calcined at 600 °C show high specific capacitance of 350 F g-1 and specific capacity of 175 C g-1 at current density of 0.3 A g-1 due to less particle agglomeration, good charge transfer and more contribution of electrochemical active sites for redox reactions. In addition, the developed supercapattery of Sr-based nanomaterials//activated carbon demonstrated high performance with maximum energy density of 21.8 Wh kg-1 and an excellent power density of 2400 W kg-1 for the lower and higher current densities. Furthermore, the supercapattery retain 87% of its capacity after continuous 3000 charge/discharge cycles. The device characteristics were further investigated by analyzing the capacitive and diffusion controlled contributions. The versatile strategy of developing mixed phased nanomaterials pave the way to synthesize other transition metal based nanomaterials with superior electrochemical performance for hybrid energy storage devices.
Related Terms
Filters
Contact Us

Please provide feedback to Administrator (afdal@afpm.org.my)

External Links