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  1. Selective dual cholinesterase inhibitors from Aconitum laeve
    Ahmad H, Ahmad S, Shah SAA, Khan HU, Khan FA, Ali M, et al.
    J Asian Nat Prod Res, 2018 Feb;20(2):172-181.
    PMID: 28463565 DOI: 10.1080/10286020.2017.1319820
    New lycoctonine-type dual cholinesterase inhibitor, swatinine-C (1), along with three known norditerpenoid alkaloids, hohenackerine (2), aconorine (5) and lappaconitine (6) and two synthetically known but phytochemically new benzene derivatives, methyl 2-acetamidobenzoate (3) and methyl 4-[2-(methoxycarbonyl)anilino]-4-oxobutanoate (4), was isolated from the roots of A. laeve. Structures of new and known compounds (1-6) were established on the basis of latest spectroscopic techniques and by close comparison with the data available in literature. In vitro, compounds (1-6) were tested against AChE and BChE inhibitory activities. Compounds 1 and 2 showed competitive inhibition against AChE (IC50 = 3.7 μM, 4.53 μM) and BChE (IC50 = 12.23 μM, 9.94 μM), respectively. Compounds 5 and 6 showed promising noncompetitive type of inhibitory profile against AChE (IC50 = 2.51 and 6.13 μM) only. Compounds 3 and 4 showed weak inhibitory profile against both AChE and BChE.
  2. Antioxidant and anticholinesterase potential of diterpenoid alkaloids from Aconitum heterophyllum
    Ahmad H, Ahmad S, Shah SAA, Latif A, Ali M, Khan FA, et al.
    Bioorg Med Chem, 2017 07 01;25(13):3368-3376.
    PMID: 28457693 DOI: 10.1016/j.bmc.2017.04.022
    Extensive chromatographic separations performed on the basic (pH=8-10) chloroform soluble fraction of Aconitum heterophyllum resulted in the isolation of three new diterpenoid alkaloids, 6β-Methoxy, 9β-dihydroxylheteratisine (1), 1α,11,13β-trihydroxylhetisine (2), 6,15β-dihydroxylhetisine (3), and the known compounds iso-atisine (4), heteratisine (5), hetisinone (6), 19-epi-isoatisine (7), and atidine (8). Structures of the isolated compounds were established by means of mass and NMR spectroscopy as well as single crystal X-ray crystallography. Compounds 1-8 were screened for their antioxidant and enzyme inhibition activities followed by in silico studies to find out the possible inhibitory mechanism of the tested compounds. This work is the first report demonstrating significant antioxidant and anticholinesterase potentials of diterpenoid alkaloids isolated from a natural source.
  3. Synthesis, SAR elucidations and molecular docking study of newly designed isatin based oxadiazole analogs as potent inhibitors of thymidine phosphorylase
    Javid MT, Rahim F, Taha M, Nawaz M, Wadood A, Ali M, et al.
    Bioorg Chem, 2018 09;79:323-333.
    PMID: 29803079 DOI: 10.1016/j.bioorg.2018.05.011
    Thymidine phosphorylase is an enzyme involved in pyrimidine salvage pathway that is identical to platelet-derived endothelial cell growth factor (PD-ECGF) and gliostatin. It is enormously up regulated in a variety of solid tumors. Furthermore, surpassing of TP level protects tumor cells from apoptosis and helps cell survival. Thus TP is identified as a prime target for developing novel anticancer therapies. A new class of exceptionally potent isatin based oxadiazole (1-30) has been synthesized and evaluated for thymidine phosphorylase inhibitory potential. All analogs showed potent thymidine phosphorylase inhibition when compared with standard 7-Deazaxanthine, 7DX (IC50 = 38.68 ± 1.12 µM). Molecular docking study was performed in order to determine the binding interaction of these newly synthesized compounds, which revealed that these synthesized compounds established stronger hydrogen bonding network with active site of residues as compare to the standard compound 7DX.
  4. Norditerpenoid alkaloids of Delphinium denudatum as cholinesterase inhibitors
    Ahmad H, Ahmad S, Ali M, Latif A, Shah SAA, Naz H, et al.
    Bioorg Chem, 2018 08;78:427-435.
    PMID: 29698893 DOI: 10.1016/j.bioorg.2018.04.008
    Three new norditerpenoids alkaloids, 1β-hydroxy,14β-acetyl condelphine (1), jadwarine-A (2), jadwarine-B (3) along with two known alkaloids isotalatizidine hydrate (4) and dihydropentagynine (5) were isolated from medicinal plant Delphinium denudatum. The structures of natural products 1-5 were established on the basis of HR-EIMS, 1H and 13C NMR (1D & 2D) spectroscopic data as well as by comparison from literature data. The structures of compound 1 and 4 were also confirmed by single crystal X-ray diffraction studies. In-vitro AChE and BChE enzyme inhibitory activities of compounds 1-5 and molecular docking studies were performed to investigate the possible molecular inhibitory mechanism of the isolated natural products. Compound 2, 4 and 5 showed competitive inhibitory effects by inhibiting AChE and BChE, respectively, while 1 and 3 showed non-competitive inhibition. This work is the first report that provides a supporting evidence about the use of constituents of Delphinium denudatum in cerebral dementia and Alzheimer diseases.
  5. 2-{[5-(Substituted-phenyl)-1,3,4-oxadiazol-2-yl]sulfanyl}-N-(1,3-thiazol-2-yl)acetamides: New bi-heterocycles as possible therapeutic agents
    Ramzan MS, Abbasi MA, Rehman A, Siddiqui SZ, Shah SAA, Ashraf M, et al.
    Pak J Pharm Sci, 2018 May;31(3(Supplementary)):1051-1059.
    PMID: 29731443
    An electrophile, N-(1,3-thiazol-2-yl)-2-bromoacetamide (3), was synthesized by the reaction of 1,3-thiazole-2-amine (1) and 2-bromoethanoyl bromide (2) in an aqueous medium. A series of carboxylic acids, 7a-j, were converted into 1,3,4-oxadiazole heterocyclic core, through a series of three steps. The final compounds, 8a-j, were synthesized by stirring 7a-j and 3 in an aprotic polar solvent. The structural elucidation of the synthesized compounds was supported by IR, EI-MS, 1H-NMR, and 13C-NMR spectral data. Title compounds were evaluated for enzyme inhibition against cholinesterases and α-glucosidase enzymes and their cytotoxic behavior was monitored using brine shrimp assay. The enzyme inhibitor potential of compounds was supported by molecular docking studies.
  6. Fulltext Frequency and predictors of anxiety and depression among pregnant women attending tertiary healthcare institutes of Quetta City, Pakistan
    Ghaffar R, Iqbal Q, Khalid A, Saleem F, Hassali MA, Baloch NS, et al.
    BMC Womens Health, 2017 Jul 25;17(1):51.
    PMID: 28743261 DOI: 10.1186/s12905-017-0411-1
    BACKGROUND: Anxiety and depression (A&D) are commonly reported among pregnant women from all over the world; however, there is a paucity of workable data from the developing countries including Pakistan. The current study, therefore, aims to find out the frequency and predictors of A&D among pregnant women attending a tertiary healthcare institutes in the city of Quetta, in the Balochistan province, Pakistan.

    METHODS: A questionnaire based, cross-sectional survey was conducted. The pre-validated Hospital Anxiety and Depression Scale (HADS) were used to assess the frequency of A&D among study respondents. Anxiety and depression scores were calculated via standard scoring procedures while logistic regression was used to identify the predictors of A&D. SPSS v. 20 was used for data analysis and p 

  7. Conventional versus microwave assisted synthesis, molecular docking and enzyme inhibitory activities of new 3,4,5-trisubstituted-1,2,4-triazole analogues
    Virk NA, Rehman A, Abbasi MA, Siddiqui SZ, Rashid U, Iqbal J, et al.
    Pak J Pharm Sci, 2018 Jul;31(4(Supplementary)):1501-1510.
    PMID: 30058542
    N-(Substituted)-5-(1-(4-methoxyphenylsulfonyl)piperidin-4-yl)-4H-1,2,4-triazol-3-ylthio) acetamide were synthesized by following conventional as well as microwave assisted protocol through five consecutive steps under the impact of various reaction conditions to control the reaction time and the yield of product. Starting from 4-methoxybenzenesulfonyl chloride and ethyl isonipecotate, product 3 was obtained which was converted into product 4 by treating with hydrazine hydrate. In step 3, the product 4 was refluxed with methyl isothiocyanate and KOH to yield compound 5 which was finally treated with variety of N-substituted acetamides to yield an array of different new compounds (8a-k). These synthesized compounds were evaluated for their inhibition potential against bovine carbonic anhydrase (bCA-II), acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. Compound 8g demonstrated good activity against bCA-II, AChE and BChE with IC50 values of 8.69 ± 0.38 μM, 11.87±0.19 μM and 26.01±0.55 μM respectively. SAR studies assisted with molecular docking were carried out to explore the mode of binding of the compounds against the studied enzymes.
  8. Synthesis, Antioxidant and In-Silico Studies of Potent Urease Inhibitors: N-(4-{[(4-Methoxyphenethyl)-(substituted)amino]sulfonyl}phenyl)acetamides
    Abbasi MA, Raza H, Rehman AU, Siddiqui SZ, Nazir M, Mumtaz A, et al.
    Drug Res (Stuttg), 2019 Feb;69(2):111-120.
    PMID: 30086567 DOI: 10.1055/a-0654-5074
    In this study, a new series of sulfonamides derivatives was synthesized and their inhibitory effects on DPPH and jack bean urease were evaluated. The in silico studies were also applied to ascertain the interactions of these molecules with active site of the enzyme. Synthesis was initiated by the nucleophilic substitution reaction of 2-(4-methoxyphenyl)-1-ethanamine (1: ) with 4-(acetylamino)benzenesulfonyl chloride (2): in aqueous sodium carbonate at pH 9. Precipitates collected were washed and dried to obtain the parent molecule, N-(4-{[(4-methoxyphenethyl)amino]sulfonyl}phenyl)acetamide (3): . Then, this parent was reacted with different alkyl/aralkyl halides, (4A-M: ), using dimethylformamide (DMF) as solvent and LiH as an activator to produce a series of new N-(4-{[(4-methoxyphenethyl)-(substituted)amino]sulfonyl}phenyl)acetamides (5A-M: ). All the synthesized compounds were characterized by IR, EI-MS, 1H-NMR, 13C-NMR and CHN analysis data. All of the synthesized compounds showed higher urease inhibitory activity than the standard thiourea. The compound 5 F: exhibited very excellent enzyme inhibitory activity with IC50 value of 0.0171±0.0070 µM relative to standard thiourea having IC50 value of 4.7455±0.0546 µM. Molecular docking studies suggested that ligands have good binding energy values and bind within the active region of taget protein. Chemo-informatics properties were evaluated by computational approaches and it was found that synthesized compounds mostly obeyed the Lipinski' rule.
  9. 2-Furoic piperazide derivatives as promising drug candidates of type 2 diabetes and Alzheimer's diseases: In vitro and in silico studies
    Abbasi MA, Hassan M, Ur-Rehman A, Siddiqui SZ, Hussain G, Shah SAA, et al.
    Comput Biol Chem, 2018 Dec;77:72-86.
    PMID: 30245349 DOI: 10.1016/j.compbiolchem.2018.09.007
    The heterocyclic compounds have been extensively reported for their bioactivity potential. The current research work reports the synthesis of some new multi-functional derivatives of 2-furoic piperazide (1; 1-(2-furoyl)piperazine). The synthesis was initiated by reacting the starting compound 1 with 3,5-dichloro-2-hydroxybenzenesulfonyl chloride (2) in a basic, polar and protic medium to obtain the parent sulfonamide 3 which was then treated with different electrophiles, 4a-g, in a polar and aprotic medium to acquire the designed molecules, 5a-g. These convergent derivatives were evaluated for their inhibitory potential against α-glucosidase, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. Acarbose was used as a reference standard for α-glucosidase inhibition while eserine for AChE and BChE inhibition. Some of the synthesized compounds were identified as promising inhibitors of these three enzymes and their bioactivity potentials were also supported by molecular docking study. The most active compounds among the synthetic analogues might be helpful in drug discovery and development for the treatment of type 2 diabetes and Alzhiemer's diseases.
  10. Synthesis of 2-Furyl[(4-aralkyl)-1-piperazinyl]methanone derivatives as suitable antibacterial agents with mild cytotoxicity
    Abbasi MA, Nazeer MM, Rehman A, Siddiqui SZ, Hussain G, Shah SA, et al.
    Pak J Pharm Sci, 2018 Nov;31(6):2477-2485.
    PMID: 30473521
    The aim of the present research work was synthesis of some 2-furyl[(4-aralkyl)-1-piperazinyl]methanone derivatives and to ascertain their antibacterial potential. The cytotoxicity of these molecules was also checked to find out their utility as possible therapeutic agents. The synthesis was initiated by reacting furyl(-1-piperazinyl)methanone (1) in N,N-dimethylformamide (DMF) and lithium hydride with different aralkyl halides (2a-j) to afford 2-furyl[(4-aralkyl)-1-piperazinyl]methanone derivatives (3a-j). The structural confirmation of all the synthesized compounds was done by IR, EI-MS, 1H-NMR and 13C-NMR spectral techniques and through elemental analysis. The results of in vitro antibacterial activity of all the synthesized compounds were screened against Gram-negative (S. typhi, E. coli, P. aeruginosa) and Gram-positive (B. subtilis, S. aureus) bacteria and were found to be decent inhibitors. Amongst the synthesized molecules, 3e showed lowest minimum inhibitory concentration MIC = 7.52±0.μg/mL against S. Typhi, credibly due to the presence of 2-bromobenzyl group, relative to the reference standard, ciprofloxacin, having MIC = 7.45±0.58μg/mL.
  11. Isolation and characterization of novel antibacterial compound from an untapped plant, Stereospermum fimbriatum
    Izyani Awang AF, Ahmed QU, Shah SAA, Jaffri JM, Ghafoor K, Uddin ABMH, et al.
    Nat Prod Res, 2020 Mar;34(5):629-637.
    PMID: 30470132 DOI: 10.1080/14786419.2018.1494170
    Stereospermum fimbriatum or locally known as "Chicha" is traditionally used for itchy skin, earache, stomachache and postpartum treatments. This study was designed to evaluate the antimicrobial potential of S. fimbriatum's stem bark against 11 pathogens and isolate its bioactive compound. Successive soxhlet extraction was conducted using n-hexane, dichloromethane (DCM) and methanol. Disc diffusion, minimum inhibitory and bactericidal concentration (MIC & MBC) assays were done to examine the antimicrobial activity. Bioassay-guided isolation was conducted on S. fimbriatum's extract. The DCM extract of stem bark (DS) was the most potent extract followed by n-hexane extract of the stem bark (NS). A novel compound was isolated and coded as C1 which demonstrated potent antibacterial effects with the MIC values as low as 3.13 µg/mL to 6.25 µg/mL, against S. epidermidis, MRSA and S. aureus. Thus, S. fimbriatum could be a potential source of antimicrobial agents for the treatment of skin infections, specifically, MRSA.
  12. Synthesis, molecular docking, dynamic simulations, kinetic mechanism, cytotoxicity evaluation of N-(substituted-phenyl)-4-{(4-[(E)-3-phenyl-2-propenyl]-1-piperazinyl} butanamides as tyrosinase and melanin inhibitors: In vitro, in vivo and in silico approaches
    Raza H, Abbasi MA, Aziz-Ur-Rehman, Siddiqui SZ, Hassan M, Abbas Q, et al.
    Bioorg Chem, 2020 01;94:103445.
    PMID: 31826809 DOI: 10.1016/j.bioorg.2019.103445
    In the current research work, different N-(substituted-phenyl)-4-{(4-[(E)-3-phenyl-2-propenyl]-1-piperazinyl}butanamides have been synthesized according to the protocol described in scheme 1. The synthesis was initiated by reacting various substituted anilines (1a-e) with 4-chlorobutanoyl chloride (2) in aqueous basic medium to give various electrophiles, 4-chloro-N-(substituted-phenyl)butanamides (3a-e). These electrophiles were then coupled with 1-[(E)-3-phenyl-2-propenyl]piperazine (4) in polar aprotic medium to attain the targeted N-(substituted-phenyl)-4-{(4-[(E)-3-phenyl-2-propenyl]-1-piperazinyl}butanamides (5a-e). The structures of all derivatives were identified and characterized by proton-nuclear magnetic resonance (1H NMR), carbon-nuclear magnetic resonance (13C NMR) and Infra-Red (IR) spectral data along with CHN analysis. The in vitro inhibitory potential of these butanamides was evaluated against Mushroom tyrosinase, whereby all compounds were found to be biologically active. Among them, 5b exhibited highest inhibitory potential with IC50 value of 0.013 ± 0.001 µM. The same compound 5b was also assayed through in vivo approach, and it was explored that it significantly reduced the pigments in zebrafish. The in silico studies were also in agreement with aforesaid results. Moreover, these molecules were profiled for their cytotoxicity through hemolytic activity, and it was found that except 5e, all other compounds showed minimal toxicity. The compound 5a also exhibited comparable results. Hence, some of these compounds might be worthy candidates for the formulation and development of depigmentation drugs with minimum side effects.
  13. 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.
  14. Synthesis and structure-activity relationship of elastase inhibiting novel ethylated thiazole-triazole acetamide hybrids: Mechanistic insights through kinetics and computational contemplations
    Butt ARS, Abbasi MA, Aziz-Ur-Rehman, Siddiqui SZ, Hassan M, Raza H, et al.
    Bioorg Chem, 2019 05;86:197-209.
    PMID: 30711702 DOI: 10.1016/j.bioorg.2019.01.040
    Keeping in mind the pharmacological importance of 2-aminothiazole and 1,2,4-triazole heterocyclic moieties, a series of novel ethylated bi-heterocyclic acetamide hybrids, 9a-p, was synthesized in a multi-step protocol. The structures of newly synthesized compounds were characterized by 1H NMR, 13C NMR, IR and EI-MS spectral studies. The inhibitory effects of these bi-heterocyclic acetamides (9a-n) were evaluated against elastase and all these molecules were identified as potent inhibitors relative to the standard used. The Kinetics mechanism was analyzed by Lineweaver-Burk plots which revealed that, 9h, inhibited elastase competitively by forming an enzyme-inhibitor complex. The inhibition constants Ki calculated from Dixon plots for this compound was 0.9 µM. The computational study was articulate with the experimental results and these ligands unveiled good binding energy values (kcal/mol). So, these molecules can be considered as promising medicinal scaffolds for the treatment of skin melanoma, wrinkle formation, uneven pigmentation, and solar elastosis.
  15. Fulltext Knowledge and practice of adolescent females about menstruation and menstruation hygiene visiting a public healthcare institute of Quetta, Pakistan
    Michael J, Iqbal Q, Haider S, Khalid A, Haque N, Ishaq R, et al.
    BMC Womens Health, 2020 01 06;20(1):4.
    PMID: 31906921 DOI: 10.1186/s12905-019-0874-3
    BACKGROUND: The current study is aimed to assess menstruation-related knowledge and practices of adolescent females visiting a public health care institute of Quetta city, Pakistan.

    METHODS: A questionnaire-based cross-sectional survey was conducted. Nine hundred and twenty three female adolescents attending general out-patient departments of Mohtarma Shaheed Benazir Bhutto Hospital Quetta, Balochistan, was approached for data collection. Based on the objectives of the study, descriptive analysis was conducted and SPSS v. 21.0 was used for the data analysis.

    RESULTS: Demographic characteristics revealed that the mean age of the respondents was 15 years. Mothers' (67%) were the main source of menstruation-related information. Majority (77.7%) of our respondents never had a class or session regarding menstruation-related education in their schools. About (44%) knew that menstruation is a physiological phenomenon while 60.2% knew that menstrual blood comes from the vagina. Nearly 40% of our study respondents missed their schools because of menarche. The use of absorbent material was frequent (90%) among the adolescent females and (68.7%) used commercially available sanitary napkins/pads. Although majority of the respondents (58.2%) were not taking baths during menstruation, 80.5% do cleaned their genitalia with water during menstruation.

    CONCLUSION: Female adolescents of our study had certain misconception regarding menstruation because of poor access to health-related education. Education can be provided at healthcare facilities, residential area as well as religious centers. Adolescent reproductive health should be included in the school curriculum; this will influence general reproductive health of females.

  16. α-Glucosidase inhibitory potential and hemolytic evaluation of newly synthesized 3,4,5-trisubstituted-1,2,4-triazole derivatives
    Nafeesa K, Aziz-Ur-Rehman -, Abbasi MA, Siddiqui SZ, Rasool S, Ali Shah SA, et al.
    Pak J Pharm Sci, 2019 Nov;32(6):2651-2658.
    PMID: 31969298
    A series of 1, 2, 4-triazole derivatives bearing piperidine moiety has been introduced as new anti-diabetic drug candidates with least cytotoxicity. p-Chlorophenylsulfonyl chloride (1) and ethyl nipecotate (2) were the starting reagents that resulted into corresponding 3,4,5-trisubstituted-1,2,4-triazole (6) through a series of steps. A series of electrophiles, 9a-e, were synthesized by reacting 4-bromobutyryl chloride (7) with differently substituted aromatic amines (8a-e) under basic aqueous medium. Target derivatives, 10a-e, were synthesized by the reaction of compound 6 with N-aryl-4-bromobutanamides (9a-e) in an aprotic solvent. Structures of all the derivatives were verified by spectroscopic analysis using IR, 1H-NMR, 13C-NMR and EIMS. Most of the derivatives revealed moderate to good α-glucosidase inhibitory activity with reference to acarbose. The moderate hemolytic potential demonstrated least toxicity.
  17. Synthesis of new S-substituted derivatives of 5-[3-(1H-indol-3-yl)propyl]-1,3,4-oxadiazol-2-ylhydrosulfide as suitable antibacterial and anticancer agents with moderate cytotoxicity
    Nazir M, Abbasi MA, Aziz-Ur-Rehman -, Siddiqui SZ, Ali Shah SA, Shahid M, et al.
    Pak J Pharm Sci, 2019 Nov;32(6):2585-2597.
    PMID: 31969290
    In the study presented here, the nucleophilic substitution reaction of 5-[3-(1H-indol-3-yl)propyl]-1,3,4-oxadiazol-2-ylhydrosulfide was carried out with different alkyl/aralkyl halides (5a-r) to form its different S-substituted derivatives (6a-r), as depicted in scheme 1. The structural confirmation of all the synthesized compounds was done by IR, 1H-NMR, 13C-NMR and CHN analysis data. Bacterial biofilm inhibitory activity of all the synthesized compounds was carried out against Bacillus subtilis and Escherichia coli. The anticancer activity of these molecules was ascertained using anti-proliferation (SRB) assay on HCT 116 Colon Cancer Cell lines while the cytotoxicity of these molecules was profiled for their haemolytic potential. From this investigation it was rational that most of the compounds exhibited suitable antibacterial and anticancer potential along with a temperate cytotoxicity.
  18. Edge AI-Based Automated Detection and Classification of Road Anomalies in VANET Using Deep Learning
    Bibi R, Saeed Y, Zeb A, Ghazal TM, Rahman T, Said RA, et al.
    Comput Intell Neurosci, 2021;2021:6262194.
    PMID: 34630550 DOI: 10.1155/2021/6262194
    Road surface defects are crucial problems for safe and smooth traffic flow. Due to climate changes, low quality of construction material, large flow of traffic, and heavy vehicles, road surface anomalies are increasing rapidly. Detection and repairing of these defects are necessary for the safety of drivers, passengers, and vehicles from mechanical faults. In this modern era, autonomous vehicles are an active research area that controls itself with the help of in-vehicle sensors without human commands, especially after the emergence of deep learning (DNN) techniques. A combination of sensors and DNN techniques can be useful for unmanned vehicles for the perception of their surroundings for the detection of tracks and obstacles for smooth traveling based on the deployment of artificial intelligence in vehicles. One of the biggest challenges for autonomous vehicles is to avoid the critical road defects that may lead to dangerous situations. To solve the accident issues and share emergency information, the Intelligent Transportation System (ITS) introduced the concept of vehicular network termed as vehicular ad hoc network (VANET) for achieving security and safety in a traffic flow. A novel mechanism is proposed for the automatic detection of road anomalies by autonomous vehicles and providing road information to upcoming vehicles based on Edge AI and VANET. Road images captured via camera and deployment of the trained model for road anomaly detection in a vehicle could help to reduce the accident rate and risk of hazards on poor road conditions. The techniques Residual Convolutional Neural Network (ResNet-18) and Visual Geometry Group (VGG-11) are applied for the automatic detection and classification of the road with anomalies such as a pothole, bump, crack, and plain roads without anomalies using the dataset from different online sources. The results show that the applied models performed well than other techniques used for road anomalies identification.
  19. Fulltext Synthesis, characterization, molecular docking and biological evaluation of Schiff Base derivatives of cefpodoxime
    Mahmood W, Ahmad I, Khan MA, Ali Shah SA, Ashraf M, Shahzad MI, et al.
    Heliyon, 2022 Nov;8(11):e11332.
    PMID: 36387450 DOI: 10.1016/j.heliyon.2022.e11332
    Synthesis of new Cefpodoxime derivatives via Schiff Bases mechanism and the efficiency of their antimicrobial and antiviral activities were addressed. They were analyzed for structural validation by using spectroscopic techniques using FTIR, 1HNMR, and 13CNMR. Molecular docking against IBV Virus papain-like protease (PLPro) was done with Auto dock tools against compounds having excellent IC50 values against IBV (Corona Class) virus. All derivatives showed strong zone of inhibition ranges from (55 ± 2.0 to 70 ± 0.8 mm) against E. coli. Compounds 1,2,4 and 6 derivatives showed remarkable activity against Stenotrophomonas maltophilia and Serratia marcescens. But For most the newly synthesized derivatives C 1 (64 ± 1.60), C 3 (32 ± 0.80), and C 8 (64 ± 1.60) showed potential IC50 values against two variants of Corona class viruses i.e. Avian Influenza (H9) and Avian corona (IBV) viruses. The current study revealed that newly synthesized Schiff Bases possessed strong anti-viral potential. Further studies may make a breakthrough in medical sciences to tackle latest challenges such as Corona Virus Diseases.
  20. Fulltext The 3D Printability and Mechanical Properties of Polyhydroxybutyrate (PHB) as Additives in Urethane Dimethacrylate (UDMA) Blends Polymer for Medical Application
    Abu Bakar AA, Zainuddin MZ, Abdullah SM, Tamchek N, Mohd Noor IS, Alauddin MS, et al.
    Polymers (Basel), 2022 Oct 25;14(21).
    PMID: 36365512 DOI: 10.3390/polym14214518
    The integration of additive manufacturing (3D printing) in the biomedical sector required material to portray a holistic characteristic in terms of printability, biocompatibility, degradability, and mechanical properties. This research aims to evaluate the 3D printability and mechanical properties of polyhydroxybutyrate (PHB) as additives in the urethane dimethacrylate (UDMA) based resin and its potential for medical applications. The printability of the PHB/UDMA resin blends was limited to 11 wt.% as it reached the maximum viscosity value at 2188 cP. Two-way analysis of variance (ANOVA) was also conducted to assess the significant effect of the varied PHB (wt.%) incorporation within UDMA resin, and the aging duration of 3D printed PHB/UDMA on mechanical properties in terms of tensile and impact properties. Meanwhile, the increasing crystallinity index (CI) of X-ray diffraction (XRD) in the 3D printed PHB/UDMA as the PHB loading increased, indicating that there is a strong correlation with the lower tensile and impact strength. FESEM images also proved that the agglomerations that occurred within the UDMA matrix had affected the mechanical performance of 3D printed PHB/UDMA. Nonetheless, the thermal stability of the 3D printed PHB/UDMA had only a slight deviation from the 3D printed UDMA since it had better thermal processability.
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