Synthesis and biological activity evaluation of a novel pleuromutilin derivative 22-((2-methyl-1-(1H-pyrrole-2-carboxamido)propan-2-yl)thio)-deoxypleuromutilin.

ABSTRACT:

Objective and methods

Widespread antibiotic misuse has resulted in growing antimicrobial resistance, diminishing the clinical efficacy of existing antibiotics against resistant strains. Therefore, we designed and synthesized a novel pleuromutilin derivative PDP, and its antibacterial activities were evaluated in vitro and in vivo.

Results

PDP exhibited potent antibacterial activity against Gram-positive bacteria (MRSA, MRSE, Staphylococcus aureus, Streptococcus agalactiae and Staphylococcus dysgalactiae), demonstrating a remarkably low MIC of 0.008 μg/mL, which was superior to both reference drugs tiamulin and valnemulin. Moreover, compared to tiamulin, it displayed a slower rate of resistance development. Molecular docking results d

SUBMITTER: Li Z 

PROVIDER: S-EPMC12447641 | biostudies-literature | 2025

REPOSITORIES: biostudies-literature