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Research in Pharmaceutical Sciences، جلد ۱۷، شماره ۱، صفحات ۹۹-۱۱۰
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عنوان انگلیسی Design, synthesis, and molecular docking of cysteine-based sulphonamide derivatives as antimicrobial agents
چکیده انگلیسی مقاله Background and purpose : The preponderance of microbial infections remains a global challenge. In the present study, synthesis of novel cysteine-based antimicrobial agents and their biological evaluation is reported. Experimental approach : The reaction of p- toluenesulphonyl chloride with cysteine afforded 2-{[(4-methylphenyl)sulphonyl]amino}-3-sulphanylpropanoic acid (3) which was acetylated based on Lumiere-Barbier method using acetic anhydride. The ammonolysis of the acetylated compound ( 4 ) gave the carboxamide derivative ( 5 ) which reacted with aniline, aminopyridine and diaminopyrimidine via nickel catalyzed Buchwald-Hartwig amidation reaction to afford compounds 6a, 6b, and 6c , respectively. The compounds were characterized using FTIR, 1 H-NMR, 13 C-NMR, and elemental analysis. The in vitro antimicrobial activities were determined. Their physicochemical properties were generated in silico and the molecular docking studied bacterial and fungal infections. Findings/Results : Compounds 4, 6b, and 6c exhibited excellent in vitro antibacterial activities while compound 4 had the best antifungal activities. From the in silico antimicrobial results, compound 3 had a better binding affinity (-10.95 kcal/mol) than penicillin (-10.89 kcal/mol) while compounds 3 and 4 had binding affinities (-10.07 and -10.62kcal/mol) comparable to ketoconazole (-10.85 kcal/mol). Conclusion and implication : All the synthesized compounds exhibited significant antibacterial and antifungal activities and were confirmed to be potential antimicrobial agents. Keywords : Antimicrobial activity; Carboxamide; Cysteine; Molecular docking; Sulphonamide.
کلیدواژه‌های انگلیسی مقاله Keywords, Antimicrobial activity,Carboxamide,Cysteine,Molecular docking,Sulphonamide.
نویسندگان مقاله | Melford C. Egbujor
2Synthetic Organic Chemistry Division, Department of Pure and Industrial Chemistry, University of Nigeria, Nsukka, Enugu State, Nigeria.


| Uchechukwu C. Okoro
3Department of Pharmaceutical and Medicinal Chemistry, University of Nigeria, Nsukka, Enugu State, Nigeria.


| Sunday N. Okafor
4Department of Pure and Industrial Chemistry, Kogi State University, Anyigba, Kogi State, Nigeria


| Samuel A. Egu
5Department of Biochemistry, Renaissance University, Ugbawka, Enugu State, Nigeria.


| Ifeanyi S. Amasiatu
6Department of Microbiology, Renaissance University, Ugbawka, Enugu State, Nigeria.


| Pius I. Egwuatu
7Department of Applied Microbiology and Brewing, Nnamdi Azikiwe University, P.M.B 5025 Awka, Anambra State, Nigeria.


| Odera R. Umeh
7Department of Applied Microbiology and Brewing, Nnamdi Azikiwe University, P.M.B 5025 Awka, Anambra State, Nigeria.


| Eziafakaego M. Ibo


نشانی اینترنتی http://rps.mui.ac.ir/index.php/jrps/article/view/2110
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زبان مقاله منتشر شده en
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نوع مقاله منتشر شده Original Article
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