Synthesis and Antimicrobial Activity of Thiophene-Based Heterocycles Derived from Thiophene-2-Carbohydrazide
Eman A. E. El‐Helw, Abdullah YA Alzahrani, Sayed K. Ramadan
Abstract
Aim: Thiophene-based heterocycles were synthesized and evaluated for their antimicrobial activity against methicillin-resistant Staphylococcus aureus, Escherichia coli, Clostridium difficile and Candida albicans strains. Methods: Antimicrobial activity was determined using the broth microdilution method. Results: Spiro–indoline–oxadiazole 17 displayed the highest activity against C. difficile while having no effects against other bacterial strains. Compounds 8 and 16 displayed strong effects against TolC, an outer membrane protein, mutant E. coli. The results of computational chemical study and outcomes of experiments were in good agreement. A molecular docking study was conducted using a molecular operating environment to simulate the binding energies of the potent compounds with D-alanine ligase protein. Conclusion: This study suggests that spiro–indoline–oxadiazole 17 could be a good anticlostridial agent.