Synthesis, Characterization, Antibacterial Evaluation, and Enzyme Inhibition Activity of a Novel Nitrogen-containing Heterocyclic Sulfonamide

Abstract

aims: Synthesis and screening of some novel sulfonamide derivatives with antibacterial and enzyme inhibitory effects. background: Currently, microbial infections are a global threat to human health and there is an urgent need to develop new and effective antimicrobial drugs to treat microbial infections. Carbonic anhydrase II is associated with a variety of diseases in vivo, and the development of carbonic anhydrase II inhibitors has far-reaching implications for the treatment of a wide range of diseases. objective: Synthesis of some novel sulfonamide derivatives containing pyrazole, 1,2,3-triazole and investigation of antimicrobial and enzyme inhibitory activities of the synthesised compounds. method: The compounds with bacteriostatic effect were screened by using the ring of inhibition method and MTT chromogenic method, and the mechanism of bacteriostatic inhibition and description of bacteriostatic effect of the synthesized compounds were investigated with the aid of MOE molecular docking simulation and Gaussian molecular weighting calculations. The in vitro inhibitory effect of the synthesized compounds on COX-2 was studied by phenylmethyl acetate colour development method. result: The results of bacterial inhibition experiments revealed that compounds 11d and 11e had better inhibition effects on pathogenic bacteria, especially on Candida albicans, which was essentially the same as that of the positive control FLUCZ. The compounds 4f, 7b and 11c were found to have the best inhibitory effect by COX-2 in vitro inhibition experiments, especially 11c, which had a better inhibitory effect than the positive control acetazolamide. conclusion: A series of derivatives obtained by introducing pyrazole and 1,2,3-triazole rings into sulfonamides have good bacteriostatic and COX-2 inhibition effects, and have the potential to be developed as novel antimicrobial agents and enzyme inhibitors. other: None other