Displaying publications 2981 - 3000 of 7301 in total

Abstract:
Sort:
  1. Halogen engineering of 4-aminoantipyrine amide derivatives for the corrosion protection of mild steel: experimental and DFT insights
    Afaq A, Aamir M, Aziz S, Woodward S, Haroon M, Sajid Z, et al.
    Phys Chem Chem Phys, 2026 Oct 27.
    PMID: 42944717 DOI: 10.1039/d6cp03224a
    Corrosion of mild steel in acidic environments is a major industrial challenge, driving the synthesis of efficient and tunable organic inhibitors. Herein, twelve halogenated 4-aminoantipyrine amide derivatives (M1-M12) were synthesized and characterized by FT-IR and NMR (1H-NMR, 13C-NMR, COSY, and HSQC) spectroscopy and HRMS. Their ability for the corrosion inhibition of mild steel in 1 M HCl was evaluated by weight loss, PDP, EIS, and SEM analyses and DFT calculations. At 1 mM, M5, M12 and M7 exhibited inhibition efficiencies (IE) of 96.46 ± 1.9%, 95.58 ± 1.9% and 94.69 ± 1.8%, respectively; M5 also exhibited the highest electrochemical efficiencies at 0.5 mM (PDP 96.51 ± 0.9% and EIS 95.70 ± 1.1%). Efficiency increased with concentration and decreased with temperature. Negative ΔG° values (-15.53 to -10.86 kJ mol-1) and the Langmuir fit indicate spontaneous, predominantly physical adsorption, possibly with specific donor-acceptor contributions. PDP showed mixed-type behaviour, and EIS showed increased charge-transfer resistance. Halogen type, substituent position and alkyl-chain length strongly influenced performance.
  2. Fulltext Divergent Effects of Palm Tocotrienol-Rich Mixture in Refined Olive Oil and Alpha-Tocopherol on Joint Health in a Rat Model of Osteoarthritis Induced with Monosodium Iodoacetate
    Al-Saadi HM, Ekeuku SO, Ahmad F, Mohamed NV, Muhammad N, Chin KY
    Pharmaceuticals (Basel), 2026 Oct 05;19(10).
    PMID: 42943277 DOI: 10.3390/ph19101580
    Background/Objectives: Palm tocotrienol-rich mixture (PT) is a potential disease-modifying agent against osteoarthritis (OA), but direct comparisons with α-tocopherol (AT) are lacking. This study evaluated the joint-protective effects of PT versus AT in a monosodium iodoacetate (MIA)-induced rat model of OA. Methods: Male Sprague-Dawley rats (n = 6/group) received intra-articular MIA in the left knees to induce OA, followed by daily oral treatment with distilled water (OA control), glucosamine sulphate (250 mg/kg), AT (100 mg/kg), or PT (100 mg/kg, in refined olive oil) for four weeks. Non-OA rats receiving distilled water served as normal controls. Body weight, joint width, and grip strength were monitored weekly. Left knees were harvested for histological evaluation using Mankin scores. Cartilage lysates from the left knees were analysed for inflammatory cytokine and metalloproteinase gene expressions, along with protein phosphorylation ratios of β-catenin (Ctnnb) and nuclear factor kappa-B (Nfkb). Results: PT-treated rats showed no significant time-dependent deterioration in joint width or grip strength over the 4-week period. Histologically, PT significantly reduced cartilage structural degradation (p = 0.002 vs. OA control) and downregulated Mmp13 mRNA expression (p < 0.05 vs. OA control). Conversely, AT upregulated Il1b (p = 0.002 vs. OA control; p = 0.010 vs. normal control), Sost (p < 0.05 vs. all OA groups), and Ctnnb (p = 0.010 vs. OA control) mRNA expressions. However, no intergroup differences in phosphorylation of Ctnnb and Nfkb were observed (p > 0.05). Conclusions: PT is associated with a chondroprotective profile in MIA-induced OA rats, whereas AT is associated with a catabolic transcriptional pattern. Nevertheless, AT did not cause significant worsening of cartilage structure or activation of pathways under these conditions.
  3. Fulltext Cytotoxic effect and apoptotic induction of tricyclohexyltin p-methoxycinnamate on HT-29 colorectal cancer cells: Implications for anticancer therapeutics
    Akim AM, Chaudhry GE, Zeenia, Ken TW, Sung YY, Tengku Muhammad TS
    J Adv Pharm Technol Res, 2025;16(1):1-5.
    PMID: 40177511 DOI: 10.4103/JAPTR.JAPTR_427_23
    Colorectal cancer's escalating prevalence in Malaysia prompts the exploration of innovative anticancer agents; amidst this backdrop, tricyclohexyltin p-methoxycinnamate emerges as a synthesized organotin complex with unique bioactive properties. Notably, the novelty of this research lies in its groundbreaking investigation into the hitherto unexplored anticancer potential and mode of cell death induced by tricyclohexyltin p-methoxycinnamate on colon cancer (human colorectal adenocarcinoma cell line (HT-29)) cell lines. This study pioneers the assessment of tricyclohexyltin p-methoxycinnamate's cytotoxic effects through the "(3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide) assay," revealing a dose- and time-dependent cytotoxicity with IC50 values of 1.2 × 10-6M for 24 h, 1.0 × 10-6M for 48 h, and 5.0 × 10-7M for 72 h. The mode of cell death through "AO/PI" staining alongside cell cycle analysis, highlighting apoptosis as the predominant mode of cell death in the HT-29 cell line, accompanied by substantial cell cycle arrest at the sub-"G0" phase. The tricyclohexyltin p-methoxycinnamate's shown potential antiproliferative properties, cell cycle arrest, and apoptosis in HT-29 cancer cells. This novel insight into the compound's mode of action positions it as a promising candidate for future anticancer therapeutics. The study underscores the urgency of investigating innovative approaches amidst the rising colorectal cancer rates, emphasizing the compound's potential through further in-depth studies and preclinical trials.
  4. Retraction notice to "Bio-inspired based meta-heuristic approach for predicting the strength of fiber-reinforced based strain hardening cementitious composites" [Heliyon 9 (2023) e21601]
    Khan Y, Zafar A, Rehman MF, Javed MF, Iftikhar B, Gamil Y
    Heliyon, 2025 Mar 20;11(6):e43082.
    PMID: 40201505 DOI: 10.1016/j.heliyon.2025.e43082
    [This retracts the article DOI: 10.1016/j.heliyon.2023.e21601.].
  5. Programmed cell death pathways and current antitumor targets
    Tan ML, Ooi JP, Ismail N, Moad AI, Muhammad TS
    Pharm Res, 2009 Jul;26(7):1547-60.
    PMID: 19407932 DOI: 10.1007/s11095-009-9895-1
    Apoptosis and autophagic cell deaths are programmed cell deaths and they play essential roles in cell survival, growth and development and tumorigenesis. The huge increase of publications in both apoptosis and autophagic signaling pathways has contributed to the wealth of knowledge in facilitating the understanding of cancer pathogenesis. Deciphering the molecular pathways and molecules involved in these pathways has helped scientists devise and develop targeted strategies against cancer. Various drugs targeting the apoptotic TRAIL, Bcl-2 and proteasome pathways are already in Phase II/III clinical trials. The first mTOR inhibitor, temsirolimus has already been approved by the FDA, USA for the treatment of advanced renal cell carcinoma and more mTOR inhibitors are expected to be in the market in a few years time. Strategizing against aberrant autophagy activities in various cancers by using either pro-autophagics or autophagy inhibitors are currently been investigated. This review aims to discuss the most recent antitumor strategies targeting the apoptosis and autophagy signaling pathways and the latest outcome of clinical trials of the above drugs.
  6. Effects of supplementing organic- and inorganic-based selenium with vitamin E on intestinal histomorphology, caecal bacterial proliferation, and short-chain fatty acid profile in layer hens
    Zainudin NN, Hemly NIM, Muhammad AI, Nayan N, Samsudin AA
    Trop Anim Health Prod, 2023 Feb 20;55(2):90.
    PMID: 36806991 DOI: 10.1007/s11250-023-03482-x
    The effects of supplementing different dietary selenium (Se) sources on intestinal histomorphology, caecal bacterial proliferation, and caecum short-chain fatty acid in layer chickens were studied. A total of 120 of 54-week-old Lohman Brown Classic laying hens were subjected to four dietary treatments: control group with no Se supplementation (T1), 0.3 mg/kg of sodium selenite (T2), 0.3 mg/kg of selenium yeast (T3), and 0.3 mg/kg of bacterial Se (Stenotrophomonas maltophilia, ADS18) (T4). All treatments were also supplemented with 250 mg/kg of vitamin E. Results showed significantly (p < 0.05) higher villus height in different small intestine parts in hens fed with diets containing organic Se sources (T3 and T4), as compared to inorganic sources (T2) and control (T1). A greater crypt depth was observed for the T1 group, as compared to T3 and T4 groups. The total bacterial populations of Bifidobacteria spp. and Lactobacilli spp. were significantly increased (p < 0.05), and tEscherichia coli population was significantly decreased (p < 0.05) in T3 and T4 groups. No effect on the total caecal short-chain fatty acid (SCFAs) content was observed. However, there was a significant increase (21.5%) of the butyric acid content in T4 group. In conclusion, organic Se supplementation, particularly bacterial organic Se, enhances intestinal histomorphology, increases the beneficial caecal bacterial proliferation, and increases butyric acid content.
  7. Cobalt-catalyzed reductive cross-coupling: a review
    Hassan S, Bilal M, Khalid S, Rasool N, Imran M, Shah AA
    Mol Divers, 2025 Oct;29(5):4787-4836.
    PMID: 39466351 DOI: 10.1007/s11030-024-11017-1
    Transition-metal-catalyzed reductive cross-coupling is highly efficient for forming C-C bonds. It earns its limelight from its application by coupling unreactive electrophilic substrates to synthesize a variety of carbon-carbon bonds with various hybridizations (sp, sp2, and sp3), late-stage functionalization, and bioactive molecules' synthesis. Reductive cross-coupling is challenging to bring selectivity but promising approach. Cobalt is comparatively more affordable than other highly efficient metals e.g., palladium and nickel but cobalt catalysis is still facing efficacy challenges. Researchers are trying to harness the maximum out of cobalt's catalytic properties. Shortly, with efficiency achieved combined with the affordability of cobalt, it will revolutionize industrial applications. This review gives insight into the core of cobalt-catalyzed reductive cross-coupling reactions with a variety of substrates forming a range of differently hybridized coupled products.
  8. Lutein reverses M2 macrophages polarization and exhibits antitumor effects on human triple-negative breast cancer cells
    Ramli RR, Muhammad SNH, Azlan M, Nurul AA, Nafi SNM, Fauzi AN
    Mol Biol Rep, 2026 Jan 16;53(1):295.
    PMID: 41543578 DOI: 10.1007/s11033-026-11445-2
    BACKGROUND: Triple-negative breast cancer (TNBC) remains a major therapeutic challenge due to the lack of established molecular targets and the presence of highly infiltrating tumor-associated macrophages (TAMs), particularly the immunosuppressive M2 phenotype that drives tumor progression. This study investigated the potential of lutein, a plant-derived carotenoid with anticancer properties, to repolarize human monocyte-derived M2 macrophages into the antitumor M1 phenotype and thereby modulate the TNBC tumor microenvironment.

    METHODS AND RESULTS: CD14 + monocytes isolated from peripheral blood mononuclear cells were differentiated into M1 or M2 macrophages using GM-CSF/IFN-γ/lipopolysaccharide or M-CSF/IL-4, respectively. Lutein's effects on macrophage polarization, cell proliferation, cell migration and cytokine secretion were evaluated using flow cytometry, MTT proliferation assays, migration assays and enzyme-linked immunosorbent assays (ELISAs) in MDA-MB-231 cells. Additionally, tumor-related protein expressions from MDA-MB-231 cells were analyzed using protein arrays. Lutein significantly reduced the proliferation and migration of MDA-MB-231 cells when co-cultured with M1/M2 macrophages compared to the untreated group. IL-4 stimulation increased the expression of M2 macrophage marker (CD206) and protumor cytokines (IL-10 and TGF-β1), but lutein effectively reduced these elevated molecules in IL-4-activated macrophages. Proteomic profiling revealed that lutein downregulated several protumor proteins (survivin, VEGF, BCL-X, M-CSF, MMP-9) and upregulated antitumor markers (FKHR and GM-CSF). Furthermore, lutein markedly reduced the secretion of proinflammatory and protumorigenic cytokines and chemokines (IL-6, IL-18BPa, CCL2, CCL8, CCL7, CCL3, CCL20, and CXCL8).

    CONCLUSION: These findings suggest that lutein reprograms M2 macrophages toward an M1-like phenotype and disrupts tumor-promoting signaling within the TNBC microenvironment, highlighting its potential as an adjunct therapeutic agent.

  9. Synthesis, in vitro and in silico studies of S-alkylated 5-(4-methoxyphenyl)-4-phenyl-4H-1,2,4-triazole-3-thiols as cholinesterase inhibitors
    Arfan M, Siddiqui SZ, Abbasi MA, Rehman A, Shah SAA, Ashraf M, et al.
    Pak J Pharm Sci, 2018 Nov;31(6 (Supplementary):2697-2708.
    PMID: 30587482
    The research was aimed to unravel the enzymatic potential of sequentially transformed new triazoles by chemically converting 4-methoxybenzoic acid via Fischer's esterification to 4-methoxybenzoate which underwent hydrazinolysis and the corresponding hydrazide (1) was cyclized with phenyl isothiocyanate (2) via 2-(4-methoxybenzoyl)-N-phenylhydrazinecarbothioamide (3); an intermediate to 5-(4-methoxyphenyl)-4-phenyl-4H-1,2,4-triazol-3-thiol (4). The electrophiles; alkyl halides 5(a-g) were further reacted with nucleophilic S-atom to attain a series of S-alkylated 5-(4-methoxyphenyl)-4-phenyl-4H-1,2,4-triazole-3-thiols 6(a-g). Characterization of synthesized compounds was accomplished by contemporary spectral techniques such as FT-IR, 1H-NMR, 13C-NMR and EI-MS. Excellent cholinesterase inhibitory potential was portrayed by 3-(n-heptylthio)-5-(4-methoxyphenyl)-4-phenyl-4H-1,2,4-triazole; 6g against AChE (IC50; 38.35±0.62μM) and BChE (IC50; 147.75±0.67μM) enzymes. Eserine (IC50; 0.04±0.01μM) was used as reference standard. Anti-proliferative activity results ascertained that derivative encompassing long straight chain substituted at S-atom of the moiety was the most potent with 4.96 % cell viability (6g) at 25μM and with 2.41% cell viability at 50μMamong library of synthesized derivatives. In silico analysis also substantiated the bioactivity statistics.
  10. Fulltext Synthesis of Chromen-4-One-Oxadiazole Substituted Analogs as Potent β-Glucuronidase Inhibitors
    Taha M, Rahim F, Ali M, Khan MN, Alqahtani MA, Bamarouf YA, et al.
    Molecules, 2019 Apr 18;24(8).
    PMID: 31003424 DOI: 10.3390/molecules24081528
    Chromen-4-one substituted oxadiazole analogs 1-19 have been synthesized, characterized and evaluated for β-glucuronidase inhibition. All analogs exhibited a variable degree of β-glucuronidase inhibitory activity with IC50 values ranging in between 0.8 ± 0.1-42.3 ± 0.8 μM when compared with the standard d-saccharic acid 1,4 lactone (IC50 = 48.1 ± 1.2 μM). Structure activity relationship has been established for all compounds. Molecular docking studies were performed to predict the binding interaction of the compounds with the active site of enzyme.
  11. Fulltext Cryptic footprints of rare earth elements on natural resources and living organisms
    Adeel M, Lee JY, Zain M, Rizwan M, Nawab A, Ahmad MA, et al.
    Environ Int, 2019 06;127:785-800.
    PMID: 31039528 DOI: 10.1016/j.envint.2019.03.022
    BACKGROUND: Rare earth elements (REEs) are gaining attention due to rapid rise of modern industries and technological developments in their usage and residual fingerprinting. Cryptic entry of REEs in the natural resources and environment is significant; therefore, life on earth is prone to their nasty effects. Scientific sectors have expressed concerns over the entry of REEs into food chains, which ultimately influences their intake and metabolism in the living organisms.

    OBJECTIVES: Extensive scientific collections and intensive look in to the latest explorations agglomerated in this document aim to depict the distribution of REEs in soil, sediments, surface waters and groundwater possibly around the globe. Furthermore, it draws attention towards potential risks of intensive industrialization and modern agriculture to the exposure of REEs, and their effects on living organisms. It also draws links of REEs usage and their footprints in natural resources with the major food chains involving plants, animals and humans.

    METHODS: Scientific literature preferably spanning over the last five years was obtained online from the MEDLINE and other sources publishing the latest studies on REEs distribution, properties, usage, cycling and intrusion in the environment and food-chains. Distribution of REEs in agricultural soils, sediments, surface and ground water was drawn on the global map, together with transport pathways of REEs and their cycling in the natural resources.

    RESULTS: Fourteen REEs (Ce, Dy, Er, Eu, Gd, Ho, La, Lu, Nd, Pr, Sm, Tb, Th and Yb) were plighted in this study. Wide range of their concentrations has been detected in agricultural soils (<15.9-249.1 μg g-1) and in groundwater (<3.1-146.2 μg L-1) at various sites worldwide. They have strong tendency to accumulate in the human body, and thus associated with kidney stones. The REEs could also perturb the animal physiology, especially affecting the reproductive development in both terrestrial and aquatic animals. In plants, REEs might affect the germination, root and shoot development and flowering at concentration ranging from 0.4 to 150 mg kg-1.

    CONCLUSIONS: This review article precisely narrates the current status, sources, and potential effects of REEs on plants, animals, humans health. There are also a few examples where REEs have been used to benefit human health. However, still there is scarce information about threshold levels of REEs in the soil, aquatic, and terrestrial resources as well as living entities. Therefore, an aggressive effort is required for global action to generate more data on REEs. This implies we prescribe an urgent need for inter-disciplinary studies about REEs in order to identify their toxic effects on both ecosystems and organisms.

  12. Synthesis of enriched boron nitride nanocrystals: A potential element for biomedical applications
    Ahmad P, Khandaker MU, Muhammad N, Rehman F, Ullah Z, Khan G, et al.
    Appl Radiat Isot, 2020 Dec;166:109404.
    PMID: 32956924 DOI: 10.1016/j.apradiso.2020.109404
    The shortcomings in Boron neutron capture therapy (BNCT) and Hyperthermia for killing the tumor cell desired for the synthesis of a new kind of material suitable to be first used in BNCT and later on enable the conditions for Hyperthermia to destroy the tumor cell. The desire led to the synthesis of large band gap semiconductor nano-size Boron-10 enriched crystals of hexagonal boron nitride (10BNNCs). The contents of 10BNNCs are analyzed with the help of x-ray photoelectron spectroscopy (XPS) and counter checked with Raman and XRD. The 10B-contents in 10BNNCs produce 7Li and 4He nuclei. A Part of the 7Li and 4He particles released in the cell is allowed to kill the tumor (via BNCT) whereas the rest produce electron-hole pairs in the semiconductor layer of 10BNNCs suggested to work in Hyperthermia with an externally applied field.
  13. Fulltext Sustainable Palm Oil-The Role of Screening and Advanced Analytical Techniques for Geographical Traceability and Authenticity Verification
    Ramli US, Tahir NI, Rozali NL, Othman A, Muhammad NH, Muhammad SA, et al.
    Molecules, 2020 Jun 25;25(12).
    PMID: 32630515 DOI: 10.3390/molecules25122927
    Palm oil production from oil palm (Elaeis guineensis Jacq.) is vital for the economy of Malaysia. As of late, sustainable production of palm oil has been a key focus due to demand by consumer groups, and important progress has been made in establishing standards that promote good agricultural practices that minimize impact on the environment. In line with the industrial goal to build a traceable supply chain, several measures have been implemented to ensure that traceability can be monitored. Although the palm oil supply chain can be highly complex, and achieving full traceability is not an easy task, the industry has to be proactive in developing improved systems that support the existing methods, which rely on recorded information in the supply chain. The Malaysian Palm Oil Board (MPOB) as the custodian of the palm oil industry in Malaysia has taken the initiative to assess and develop technologies that can ensure authenticity and traceability of palm oil in the major supply chains from the point of harvesting all the way to key downstream applications. This review describes the underlying framework related to palm oil geographical traceability using various state-of-the-art analytical techniques, which are also being explored to address adulteration in the global palm oil supply chain.
  14. Fulltext Effects of Grafting on Morphophysiological and Yield Characteristic of Eggplant (Solanum melongena L.) Grafted onto Wild Relative Rootstocks
    Musa I, Rafii MY, Ahmad K, Ramlee SI, Md Hatta MA, Oladosu Y, et al.
    Plants (Basel), 2020 Nov 15;9(11).
    PMID: 33203189 DOI: 10.3390/plants9111583
    Grafting is regarded as an integral component of sustainable vegetable production. It is important in the management of soil-borne diseases, and reports suggest that grafting with viable rootstocks can enhance crop growth and yield. This research was conducted using splices and cleft grafting techniques to investigate graft compatibility among varieties of high yielding eggplant scion (MCV1, MCV2, CCV1, CCV2, CCV3, NCV, and TCV) grafted onto wild rootstocks (MWR, BWR, and TWR) to study their morphophysiological and yield characteristics. High yielding scions grafted onto wild relative rootstocks were compared with two controls including self-grafted and non-grafted. All the scion had a high rate of germination (≥95%) and remarkable graft success (100%) was recorded in MCV1, MCV2, and TCV using the cleft techniques. Generally, the use of rootstocks resulted in higher total and marketable fruit yield compared to the non-grafted and self-grafted scion plants, respectively. In particular, MWR and TWR rootstock conferred the highest vigour to the scion, resulting in the highest values recorded for total and marketable fruit yield, number of fruits per plant and average fruit weight. A similar result was obtained in fruit length and diameter, where long and wide fruits were observed in scions grafted onto MWR and TWR rootstocks, respectively. Grafting of high yielding eggplant scion onto resistant MWR, BWR and TWR eggplant rootstock was found to be beneficial for eggplant cultivation. The remarkable compatibility and vigour of the rootstock with scion led to the improvement in total and marketable yield of the fruits. As such, it can be concluded that the use of wild relative rootstocks of eggplant species can be a valuable method of improving eggplant production.
  15. Social support among older adults in Malaysia
    Mahmud MA, Hazrin M, Muhammad EN, Mohd Hisyam MF, Awaludin SM, Abdul Razak MA, et al.
    Geriatr Gerontol Int, 2020 Dec;20 Suppl 2:63-67.
    PMID: 33370852 DOI: 10.1111/ggi.14033
    AIM: This study aimed to determine the factors that influence perceived social support among older adults in Malaysia.

    METHODS: We used the 11-item Duke Social Support Index to assess perceived social support through a face-to-face interview. Higher scores indicate better social support. Linear regression analysis was carried out to determine the factors that influence perceived social support by adapting the conceptual model of social support determinants and its impact on health.

    RESULTS: A total of 3959 respondents aged ≥60 years completed the Duke Social Support Index. The estimated mean Duke Social Support Index score was 27.65 (95% CI 27.36-27.95). Adjusted for confounders, the factors found to be significantly associated with social support among older adults were monthly income below RM1000 (-0.8502, 95% CI -1.3523, -0.3481), being single (-0.5360, 95% CI -0.8430, -0.2290), no depression/normal (2.2801, 95% CI 1.6666-2.8937), absence of activities of daily living (0.9854, 95% CI 0.5599-1.4109) and dependency in instrumental activities of daily living (-0.3655, 95% CI -0.9811, -0.3259).

    CONCLUSION: This study found that low income, being single, no depression, absence of activities of daily living and dependency in instrumental activities of daily living were important factors related to perceived social support among Malaysian older adults. Geriatr Gerontol Int 2020; 20: 63-67.

  16. Fulltext One Pot Selective Arylation of 2-Bromo-5-Chloro Thiophene; Molecular Structure Investigation via Density Functional Theory (DFT), X-ray Analysis, and Their Biological Activities
    Rasool N, Kanwal A, Rasheed T, Ain Q, Mahmood T, Ayub K, et al.
    Int J Mol Sci, 2016;17(7).
    PMID: 27367666 DOI: 10.3390/ijms17070912
    Synthesis of 2,5-bisarylthiophenes was accomplished by sequential Suzuki cross coupling reaction of 2-bromo-5-chloro thiophenes. Density functional theory (DFT) studies were carried out at the B3LYP/6-31G(d, p) level of theory to compare the geometric parameters of 2,5-bisarylthiophenes with those from X-ray diffraction results. The synthesized compounds are screened for in vitro bacteria scavenging abilities. At the concentration of 50 and 100 μg/mL, compounds 2b, 2c, 2d, 3c, and 3f with IC50-values of 51.4, 52.10, 58.0, 56.2, and 56.5 μg/mL respectively, were found most potent against E. coli. Among all the synthesized compounds 2a, 2d, 3c, and 3e with the least values of IC50 77, 76.26, 79.13 μg/mL respectively showed significant antioxidant activities. Almost all of the compounds showed good antibacterial activity against Escherichia coli, whereas 2-chloro-5-(4-methoxyphenyl) thiophene (2b) was found most active among all synthesized compound with an IC50 value of 51.4 μg/mL. All of the synthesized compounds were screened for nitric oxide scavenging activity as well. Frontier molecular orbitals (FMOs) and molecular electrostatic potentials of the target compounds were also studied theoretically to account for their relative reactivity.
  17. Synthesis and molecular modelling studies of phenyl linked oxadiazole-phenylhydrazone hybrids as potent antileishmanial agents
    Taha M, Ismail NH, Imran S, Anouar EH, Selvaraj M, Jamil W, et al.
    Eur J Med Chem, 2017 Jan 27;126:1021-1033.
    PMID: 28012342 DOI: 10.1016/j.ejmech.2016.12.019
    Molecular hybridization yielded phenyl linked oxadiazole-benzohydrazones hybrids 6-35 and were evaluated for their antileishmanial potentials. Compound 10, a 3,4-dihydroxy analog with IC50 value of 0.95 ± 0.01 μM, was found to be the most potent antileishmanial agent (7 times more active) than the standard drug pentamidine (IC50 = 7.02 ± 0.09 μM). The current series 6-35 conceded in the identification of thirteen (13) potent antileishmanial compounds with the IC50 values ranging between 0.95 ± 0.01-78.6 ± 1.78 μM. Molecular docking analysis against pteridine reductase (PTR1) were also performed to probe the mode of action. Selectivity index showed that compounds with higher number of hydroxyl groups have low selectivity index. Theoretical stereochemical assignment was also done for certain derivatives by using density functional calculations.
  18. Synthesis of alpha amylase inhibitors based on privileged indole scaffold
    Noreen T, Taha M, Imran S, Chigurupati S, Rahim F, Selvaraj M, et al.
    Bioorg Chem, 2017 06;72:248-255.
    PMID: 28482265 DOI: 10.1016/j.bioorg.2017.04.010
    Twenty five derivatives of indole carbohydrazide (1-25) had been synthesized. These compounds were characterized using 1H NMR and EI-MS, and further evaluated for their α-amylase inhibitory potential. The analogs (1-25) showed varying degree of α-amylase inhibitory potential. ranging between 9.28 and 599.0µM when compared with standard acarbose having IC50 value 8.78±0.16µM. Six analogs, 25 (IC50=9.28±0.153µM), 22 (IC50=9.79±0.43µM), 4 (IC50=11.08±0.357µM), 1 (IC50=12.65±0.169µM), 8 (IC50=21.37±0.07µM) and 14 (IC50=43.21±0.14µM) showed potent α-amylase inhibition as compared to the standard acarbose (IC50=8.78±0.16µM). All other analogs displayed good to moderate inhibitory potential. Structure-activity relationship was established through the interaction of the active compounds with enzyme active site with the help of docking studies.
  19. Fulltext Synthesis, Surface Nitriding and Characterization of Ti-Nb Modified 316L Stainless Steel Alloy Using Powder Metallurgy
    Ali S, Irfan M, Muhammad Niazi U, Rani AMA, Shah I, Legutko S, et al.
    Materials (Basel), 2021 Jun 13;14(12).
    PMID: 34199244 DOI: 10.3390/ma14123270
    The powder metallurgy (PM) technique has been widely used for producing different alloy compositions by the addition of suitable reinforcements. PM is also capable of producing desireable mechanical and physical properties of the material by varying process parameters. This research investigates the addition of titanium and niobium in a 316L stainless steel matrix for potential use in the biomedical field. The increase of sintering dwell time resulted in simultaneous sintering and surface nitriding of compositions, using nitrogen as the sintering atmosphere. The developed alloy compositions were characterized using OM, FESEM, XRD and XPS techniques for quantification of the surface nitride layer and the nitrogen absorbed during sintering. The corrosion resistance and cytotoxicity assessments of the developed compositions were carried out in artificial saliva solution and human oral fibroblast cell culture, respectively. The results indicated that the nitride layer produced during sintering increased the corrosion resistance of the alloy and the developed compositions are non-cytotoxic. This newly developed alloy composition and processing technique is expected to provide a low-cost solution to implant manufacturing.
  20. Fulltext Historical and current distribution ranges and loss of mega-herbivores and carnivores of Asia
    Mahmood T, Vu TT, Campos-Arceiz A, Akrim F, Andleeb S, Farooq M, et al.
    PeerJ, 2021;9:e10738.
    PMID: 33628635 DOI: 10.7717/peerj.10738
    Ecosystem functioning is dependent a lot on large mammals, which are, however, vulnerable and facing extinction risks due to human impacts mainly. Megafauna of Asia has been declining for a long, not only in numbers but also in their distribution ranges. In the current study, we collected information on past and current occurrence and distribution records of Asia's megafauna species. We reconstructed the historical distribution ranges of the six herbivores and four carnivores for comparison with their present ranges, to quantify spatially explicit levels of mega-defaunation. Results revealed that historically the selected megafauna species were more widely distributed than at current. Severe range contraction was observed for the Asiatic lion, three rhino species, Asian elephant, tigers, and tapirs. Defaunation maps generated have revealed the vanishing of megafauna from parts of the East, Southeast, and Southwest Asia, even some protected Areas losing up to eight out of ten megafaunal species. These defaunation maps can help develop future conservation policies, to save the remaining distribution ranges of large mammals.
Related Terms
Filters
Contact Us

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

External Links