title: Synthesis and antibacterial evaluation of novel pleuromutilin derivatives.
abstract: A series of novel pleuromutilin derivatives possessing thioether moiety has been synthesized via acylation reaction under mild conditions. Their in vitro antibacterial activity against methicillin-resistant Staphylococcus aureus, methicillin-resistant Staphylococcus epidermidis, Escherichia coli, and Streptococcus agalactiae were tested by agar dilution method and Oxford cup assay. Among the 17 compounds screened, 14-O-[(4-methoxybenzamide-2- methylpropane-2-yl) thioacetate] mutilin 4i, 14-O-[(2-aminobenzamide-2-methylpropane-2-yl) thioacetate] mutilin 5a and 14-O-[(4-aminobenzamide-2-methylpropane-2-yl) thioacetate] mutilin 5c were resulted as most active antibacterial agents.
authors.affiliation: Key Laboratory of New Animal Drug Project, Gansu Province, Ministry of Agriculture, Lanzhou Institute of Animal Science and Veterinary Pharmaceutics Science, Chinese Academy of Agricultural Sciences, Jiangouyan, Qilihe District, Lanzhou 730050, PR China. shangrf1974@163.com
authors.forename: Ruofeng
authors.initials: R
authors.lastname: Shang
authors.forename: Yu
authors.initials: Y
authors.lastname: Liu
authors.forename: Zhijun
authors.initials: Z
authors.lastname: Xin
authors.forename: Wenzhu
authors.initials: W
authors.lastname: Guo
authors.forename: Zhiting
authors.initials: Z
authors.lastname: Guo
authors.forename: Baocheng
authors.initials: B
authors.lastname: Hao
authors.forename: Liang
authors.initials: L
authors.lastname: Jianping
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001549:Benzamides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D004224:Diterpenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D004926:Escherichia coli / Q000187:drug effects; D016106:Methicillin Resistance / Q000187:drug effects; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D008956:Models, Chemical; D015394:Molecular Structure; D011083:Polycyclic Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013212:Staphylococcus epidermidis / Q000187:drug effects; D013292:Streptococcus agalactiae / Q000187:drug effects; D000097567:Pleuromutilins
chemical_list: D000900:Anti-Bacterial Agents; D001549:Benzamides; D004224:Diterpenes; D011083:Polycyclic Compounds; D000097567:Pleuromutilins; C584483:14-O-((4-aminobenzamide-2-methylpropane-2-yl)thioacetate)mutilin