A series of novel N‐(substituted‐benzyl)‐4‐(trifluoromethyl)thiazole‐2‐sulfonamide (4a‐4i) and 2‐(N‐[2‐chlorobenzyl]sulfamoyl)thiazole‐4‐carboxylic acid (7a‐7i) derivatives were synthesized from readily available 4‐(trifluoromethyl)thiazol‐2‐amine (1) and ethyl 2‐aminothiazole‐4‐carboxylate (5), respectively. Eighteen novel thiazole‐2‐sulfonamide derivatives were synthesized. The targets were synthesized through a series of reactions involving diazotization and sulfonamide coupling reactions. All the synthesized compounds were characterized by 1H NMR, 19F, 13C NMR, HRMS, and HPLC analytical techniques. All the synthetic derivatives were evaluated for their antimicrobial activity (minimum inhibitory concentration) against a series of strains of Bacillus subtillis, Staphylococcus aureus, and Escherichia coli for antibacterial activity and against the strains of Candida albicans, Aspergillus flavus, and Aspergillus niger for antifungal activity. Also synthetic derivatives were tested for their in vitro anti‐tubercular (Mycobacterium tuberculosis: H37 Rv, MDR, and XDR strains) activities. Most of compounds showed moderate to good activity for antimicrobial and anti‐tubercular strains. The compounds 4b (MIC = 12.5 μg/ml and 3.125 μM), 4c (MIC = 1.562 μM), 4d (MIC = 12.5 μg/ml), 7b (MIC = 12.5 μg/ml), 7c (MIC = 26 μg/ml and 1.562 μM), and 7i (MIC = 26 μg/ml and 6.25 μM) showed good antimicrobial and anti‐tubercular activity in the range of (MIC = 12.5–26 μg/ml) and (MIC = 1.562–6.25 μM) against tested strains, while some derivatives show moderate inhibitions through the series.
A new series of 2‐(4‐(benzo[d]thiazol‐5‐ylsulfonyl)piperazin‐1‐yl)‐N‐substituted acetamide (5a‐5k) compounds have been synthesized, and these compounds were characterized with spectral data like IR, NMR, and Mass spectroscopy. All compounds were evaluated in vitro for their efficacy as antimicrobial against Gram‐positive and Gram‐negative pathogenic bacterial strains such as Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa using ciprofloxacin as a standard and fungal strains like Candida albicans and Aspergillus fumigatus as compared with standard drug Clotrimazole, and Molecular docking study shows that all these compounds were having good to excellent correlation binding energy as compared with binding energy of standard drugs.
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