Synthesis and antimicrobial activity of thiophene-based heterocycles derived from thiophene-2-carbohydrazide
El-Helw, Eman AE; Alzahrani, Abdullah Ya; Sayed Karam Ramadan Emam;
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.
Other data
Title | Synthesis and antimicrobial activity of thiophene-based heterocycles derived from thiophene-2-carbohydrazide | Authors | El-Helw, Eman AE; Alzahrani, Abdullah Ya; Sayed Karam Ramadan Emam | Keywords | DFT;anticlostridial drugs;antimicrobial;in silico studies;molecular docking;thiophene | Issue Date | 6-Feb-2024 | Journal | Future medicinal chemistry | ISSN | 1756-8919 1756-8927 |
DOI | 10.4155/fmc-2023-0304 | PubMed ID | 38318668 |
Recommend this item
Similar Items from Core Recommender Database
Items in Ain Shams Scholar are protected by copyright, with all rights reserved, unless otherwise indicated.