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Synthesis and biological evaluation of new pleuromutilin derivatives as antibacterial agents.

ABSTRACT: Several pleuromutilin derivatives possessing thiadiazole moieties were synthesized via acylation reactions under mild conditions. The in vitro antibacterial activities of the derivatives against methicillin-resistant S. aureus, methicillin-resistant S. epidermidis, S. aureus, S. epidermidis, E. coli, and B. cereus were tested by the agar dilution method and Oxford cup assay. All the screened compounds displayed potent activity. Compound 6d was the most active antibacterial agent because of its lowest MIC value and largest inhibition zone. Docking experiments were performed to understand the possible mode of the interactions between the derivatives and 50S ribosomal subunit. Moreover, the absorption, distribution, metabolism, excretion and toxicity properties of the synthesized compounds were analyzed after prediction using the Advanced Chemistry Development/Percepta Platform available online.

SUBMITTER: Shang RF

PROVIDER: S-EPMC6271455 | biostudies-literature | 2014 Nov

REPOSITORIES: biostudies-literature

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Synthesis and biological evaluation of new pleuromutilin derivatives as antibacterial agents.

Shang Ruo-Feng RF Wang Guan-Hua GH Xu Xi-Ming XM Liu Si-Jie SJ Zhang Chao C Yi Yun-Peng YP Liang Jian-Ping JP Liu Yu Y

Molecules (Basel, Switzerland) 20141119 11

Several pleuromutilin derivatives possessing thiadiazole moieties were synthesized via acylation reactions under mild conditions. The in vitro antibacterial activities of the derivatives against methicillin-resistant S. aureus, methicillin-resistant S. epidermidis, S. aureus, S. epidermidis, E. coli, and B. cereus were tested by the agar dilution method and Oxford cup assay. All the screened compounds displayed potent activity. Compound 6d was the most active antibacterial agent because of its l ...[more]

PMID: 25415471

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