title: 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.
authors.affiliation: Key Laboratory of New Animal Drug Project of Gansu Province, Key Laboratory of Veterinary Pharmaceutical Development, Lanzhou Institute of Husbandry and Pharmaceutical Sciences of CAAS, Ministry of Agriculture, Lanzhou 730050, China. shangrf1974@163.com.
authors.forename: Ruo-Feng
authors.initials: RF
authors.lastname: Shang
authors.affiliation: School of Public Health, Lanzhou University, Lanzhou 730000, China. wgh2650@163.com.
authors.forename: Guan-Hua
authors.initials: GH
authors.lastname: Wang
authors.affiliation: Department of Toxicology, School of Public Health, Guiyang Medical University, Guiyang 550004, China. xmngxu@gmail.com.
authors.forename: Xi-Ming
authors.initials: XM
authors.lastname: Xu
authors.affiliation: College of Chemical Engineering, Shijiazhuang University, Shijiazhuang 050035, China. liusijie1982@163.com.
authors.forename: Si-Jie
authors.initials: SJ
authors.lastname: Liu
authors.affiliation: Key Laboratory of New Animal Drug Project of Gansu Province, Key Laboratory of Veterinary Pharmaceutical Development, Lanzhou Institute of Husbandry and Pharmaceutical Sciences of CAAS, Ministry of Agriculture, Lanzhou 730050, China. YJL.BZN@163.com.
authors.forename: Chao
authors.initials: C
authors.lastname: Zhang
authors.affiliation: Key Laboratory of New Animal Drug Project of Gansu Province, Key Laboratory of Veterinary Pharmaceutical Development, Lanzhou Institute of Husbandry and Pharmaceutical Sciences of CAAS, Ministry of Agriculture, Lanzhou 730050, China. yiyp@foxmail.com.
authors.forename: Yun-Peng
authors.initials: YP
authors.lastname: Yi
authors.affiliation: Key Laboratory of New Animal Drug Project of Gansu Province, Key Laboratory of Veterinary Pharmaceutical Development, Lanzhou Institute of Husbandry and Pharmaceutical Sciences of CAAS, Ministry of Agriculture, Lanzhou 730050, China. Liangjp100@sina.com.
authors.forename: Jian-Ping
authors.initials: JP
authors.lastname: Liang
authors.affiliation: Key Laboratory of New Animal Drug Project of Gansu Province, Key Laboratory of Veterinary Pharmaceutical Development, Lanzhou Institute of Husbandry and Pharmaceutical Sciences of CAAS, Ministry of Agriculture, Lanzhou 730050, China. liuyu8108@163.com.
authors.forename: Yu
authors.initials: Y
authors.lastname: Liu
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects*; D004224:Diterpenes / Q000138:chemical synthesis / Q000494:pharmacology; D008826:Microbial Sensitivity Tests / Q000379:methods; D062105:Molecular Docking Simulation; D011083:Polycyclic Compounds; D000097567:Pleuromutilins
chemical_list: D000900:Anti-Bacterial Agents; D004224:Diterpenes; D011083:Polycyclic Compounds; D000097567:Pleuromutilins