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Design, synthesis, and molecular docking of cysteine-based sulphonamide derivatives as antimicrobial agents.


ABSTRACT:

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 u

SUBMITTER: Egbujor MC 

PROVIDER: S-EPMC8621839 | biostudies-literature | 2022 Feb

REPOSITORIES: biostudies-literature