Alternative approaches utilizing click chemistry to develop next-generation analogs of solithromycin.

ABSTRACT: The marked rise in bacterial drug resistance has created an urgent need for novel antibacterials belonging to new drug classes and ideally possessing new mechanisms of action. The superior biological activity of solithromycin against streptococci and other bacteria causative of community-acquired pneumonia pathogens, compared to telithromycin and other macrolides encouraged us to extensively explore this class of antibiotics. We, thus, present the design and synthesis of a novel series of solithromycin analogs. Three main strategies were pursued in structure-activity relationship studies covering the N-11 side chain and the desosamine motif, which are both chief elements for establishing strong interactions with the bacterial ribosome as the molecular target. Minimal inhibitory concentrati

SUBMITTER: Daher SS 

PROVIDER: S-EPMC9009214 | biostudies-literature | 2022 Apr

REPOSITORIES: biostudies-literature