Synthesis and Biological Evaluation of Sulfamoyl Carboxamide Derivatives from Sulfur-containing α-Amino acids

Abstract

acids and sulfonyl chloride. The characterization of the compounds was done using FTIR, 1H-NMR, 13C-NMR, and elemental analysis. Their antioxidant, antimalarial, antimicrobial activities and molecular docking were evaluated. Compounds 5h (MIC, 0.3, 0.5, 0.3 and 0.4 mg/mL) was the most potent antibacterial agent against Staphylococcus aureus, Escherichia coli, Bacillus subtilis and Salmonella typhi, compounds 5a (MIC, 0.7 mg/mL) and 5g (MIC, 0.7m g/mL) were most potent against Pseudomonas aeruginosa while compound 5e (MIC, 0.5 and 0.8 mg/mL) had the best in vitro antifungal activity against Aspergillus niger and Candida albicans. Compound 5d (1C50 = 1.128 μg/mL) displayed an antioxidant activity comparable with ascorbic acid (1C50 = 1.000 μg/mL) and compound 5e (4, 14, 4%) effected the most signifi cant reduction in the percentage malaria parasitaemia comparable with artemeter lumefantrin (5, 4, 4%) after 5 days of treatment of the mice. From the molecular docking results, compound 5c had a strong molecular interaction with the appropriate drug target, Escherichia coli DNA gyrase complexed with 1-ethyl-3-[8-methyl-5-(2-methyl-pyridin-4-yl) isoquinolin-3-yl]urea (PDB code: 5MMN). The title compounds displayed signifi cant antimicrobial, antioxidant and antimalarial activities.