Synthesis and evaluation of dual-action kanglemycin-fluoroquinolone hybrid antibiotics.

ABSTRACT: Bacterial resistance threatens the utility of currently available antibiotics. Rifampicin, a cornerstone in the treatment of persistent Gram-positive infections, is prone to the development of resistance resulting from single point mutations in the antibiotic's target, RNA polymerase. One strategy to circumvent resistance is the use of 'hybrid' antibiotics consisting of two covalently linked antibiotic entities. These compounds generally have two distinct cellular targets, reducing the probability of resistance development and potentially providing simplified pharmacological properties compared to combination therapies using the individual antibiotics. Here we evaluate a series of semi-synthetic hybrid antibiotics formed by linking kanglemycin A (Kang A), a rifampicin analog, and a collect

SUBMITTER: Peek J 

PROVIDER: S-EPMC8779240 | biostudies-literature | 2022 Feb

REPOSITORIES: biostudies-literature