biostudies-literatureUnknown16Li Z<h4>Objective and methods</h4>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 <b>PDP</b>, and its antibacterial activities were evaluated <i>in vitro</i> and <i>in vivo</i>.<h4>Results</h4><b>PDP</b> exhibited potent antibacterial activity against Gram-positive bacteria (MRSA, MRSE, <i>Staphylococcus aureus, Streptococcus agalactiae</i> and <i>Staphylococcus dysgalactiae</i>), 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 dFrontiers in pharmacology1657973https://www.ebi.ac.uk/biostudies/studies/S-EPMC12447641biostudies-literatureSynthesis and biological activity evaluation of a novel pleuromutilin derivative 22-((2-methyl-1-(1H-pyrrole-2-carboxamido)propan-2-yl)thio)-deoxypleuromutilin.PMC12447641Li ZLi JGe WQin ZBai LLiu CMa DXu XfalseSynthesis and biological activity evaluation of a novel pleuromutilin derivative 22-((2-methyl-1-(1H-pyrrole-2-carboxamido)propan-2-yl)thio)-deoxypleuromutilin.<h4>Objective and methods</h4>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 <b>PDP</b>, and its antibacterial activities were evaluated <i>in vitro</i> and <i>in vivo</i>.<h4>Results</h4><b>PDP</b> exhibited potent antibacterial activity against Gram-positive bacteria (MRSA, MRSE, <i>Staphylococcus aureus, Streptococcus agalactiae</i> and <i>Staphylococcus dysgalactiae</i>), 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 d2025-01-01T00:00:00Z20252026-06-03T17:18:13.995Z2026-04-29T03:12:59.657ZS-EPMC124476414097846310.3389/fphar.2025.1657973