Development of Penicillin-Based Carbonic Anhydrase Inhibitors Targeting Multidrug-Resistant <i>Neisseria gonorrhoeae</i>.

ABSTRACT: The development of antibacterial drugs with new mechanisms of action is crucial in combating the rise of antibiotic-resistant infections. Bacterial carbonic anhydrases (CAs, EC 4.2.1.1) have been validated as promising antibacterial targets against pathogens such as Helicobacter pylori, Neisseria gonorrhoeae, and vancomycin-resistant enterococci. A multitarget strategy is proposed to design penicillin-based CA inhibitor hybrids for tackling resistance by targeting multiple bacterial pathways, thereby resensitizing drug-resistant strains to clinical antibiotics. The sulfonamide derivatives potently inhibited the CAs from N. gonorrhoeae and Escherichia coli with K_I values in the range of 7.1-617.2 nM. Computational simulations with the main penic

SUBMITTER: Bonardi A 

PROVIDER: S-EPMC12171872 | biostudies-literature | 2024 Jun

REPOSITORIES: biostudies-literature