Discovery of new antimicrobial thiophene derivatives with activity against drug-resistant Gram negative-bacteria.

ABSTRACT: Our aim is to identify new small molecules with antimicrobial potential, especially against colistin-resistant (Col-R) Acinetobacter baumannii and Escherichia coli. After initial hits identification by fingerprint similarity, MIC of 24 heterocyclic derivatives for A. baumannii and E. coli reference strains, and bactericidal activity of selected thiophenes against Col-R strains were determined. We analyzed changes in bacterial membrane permeability and the OMPs profile. Additionally, we determined bacterial adherence to host cells and performed molecular docking studies to assess their binding to bacterial targets. The compounds' MICs ranged from 4 to >64 mg/L. Thiophene derivatives 4, 5 and 8 exhibited MIC₅₀ values between 16 and

SUBMITTER: Molina-Panadero I 

PROVIDER: S-EPMC11368766 | biostudies-literature | 2024

REPOSITORIES: biostudies-literature