A new class of nifuroxazide analogues: Synthesis of 5-nitrothiophene derivatives with antimicrobial activity against multidrug-resistant Staphylococcus aureus

Hospital-acquired methicillin-resistant Staphylococcus aureus (MRSA) has been an increasing problem worldwide since the initial reports over 40 years ago. To examine new drug leads with potential antibacterial activities, 14 p-substituted benzoic acid [(5-nitro-thiophen-2-yl)-methylene]-hydrazides were designed, synthesized, and tested against standard and multidrug-resistant S. aureus strains by serial dilution tests. All compounds exhibited significant bacteriostatic activity and some of them also showed bactericidal activity. The results confirmed the potential of this class of compounds as an alternative for the development of selective antimicrobial agents.

In this study it was evaluated the antibacterial activity of 14 acid [(5-nitro-thiophen-2-yl)-methylene]-hydrazides (Fig. 1) against multidrug-resistant (3SP/R33) Staphylococcus aureus strain. Compounds were designed according to physicochemical properties and all of them exhibited significant bacteriostatic activity. It was observed bactericidal activity for some compounds tested. These new compounds confirming the potential of nifuroxazide analogs as antimicrobial agents and represent an alternative for the development of promising antibacterial drugs.Figure optionsDownload as PowerPoint slide