title: Chemical synthesis and biological activities of novel pleuromutilin derivatives with substituted amino moiety.
abstract: Novel pleuromutilin derivatives designed based on the structure of valnemulin were synthesized and evaluated for their in vitro antibacterial activities. These pleuromutilin derivatives with substituted amino moiety exhibited excellent activities against methicillin-resistant Staphylococcus aureus, methicillin-resistant Staphylococcus epidermidis, Escherichia coli, and Streptococcus agalactiae. Compound 5b showed the highest antibacterial activities and even exceeded tiamulin. Moreover, the docking experiments provided information about the binding model between the synthesized compounds and peptidyl transferase center (PTC) of 23S rRNA.
authors.affiliation: Key Laboratory of New Animal Drug Project of Gansu Province, Key Laboratory of Veterinary Pharmacceutical Development, Ministry of Agriculture, Lanzhou Institute of Animal Science and Veterinary Pharmaceutics Science, Chinese Academy of Agricultural Sciences, Lanzhou, Gansu, China.
authors.forename: Ruofeng
authors.initials: R
authors.lastname: Shang
authors.affiliation: University Hospital of Gansu Traditional Chinese Medicine, Lanzhou, Gansu, China.
authors.forename: Shengyu
authors.initials: S
authors.lastname: Wang
authors.affiliation: Université Paris Diderot, Sorbonne Paris Cité, Unité de Biologie Fonctionnelle et Adaptative, CNRS, Paris, France.
authors.forename: Ximing
authors.initials: X
authors.lastname: Xu
authors.affiliation: Key Laboratory of New Animal Drug Project of Gansu Province, Key Laboratory of Veterinary Pharmacceutical Development, Ministry of Agriculture, Lanzhou Institute of Animal Science and Veterinary Pharmaceutics Science, Chinese Academy of Agricultural Sciences, Lanzhou, Gansu, China.
authors.forename: Yunpeng
authors.initials: Y
authors.lastname: Yi
authors.affiliation: Key Laboratory of New Animal Drug Project of Gansu Province, Key Laboratory of Veterinary Pharmacceutical Development, Ministry of Agriculture, Lanzhou Institute of Animal Science and Veterinary Pharmaceutics Science, Chinese Academy of Agricultural Sciences, Lanzhou, Gansu, China.
authors.forename: Wenzhu
authors.initials: W
authors.lastname: Guo
authors.affiliation: Key Laboratory of New Animal Drug Project of Gansu Province, Key Laboratory of Veterinary Pharmacceutical Development, Ministry of Agriculture, Lanzhou Institute of Animal Science and Veterinary Pharmaceutics Science, Chinese Academy of Agricultural Sciences, Lanzhou, Gansu, China.
authors.lastname: Yuliu
authors.affiliation: Key Laboratory of New Animal Drug Project of Gansu Province, Key Laboratory of Veterinary Pharmacceutical Development, Ministry of Agriculture, Lanzhou Institute of Animal Science and Veterinary Pharmaceutics Science, Chinese Academy of Agricultural Sciences, Lanzhou, Gansu, China.
authors.forename: Jianping
authors.initials: J
authors.lastname: Liang
mesh_terms: D000588:Amines / Q000737:chemistry*; D001665:Binding Sites; D018360:Crystallography, X-Ray; D004224:Diterpenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D004926:Escherichia coli / Q000187:drug effects; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D062105:Molecular Docking Simulation; D011083:Polycyclic Compounds; D013212:Staphylococcus epidermidis / Q000187:drug effects; D013292:Streptococcus agalactiae / Q000187:drug effects; D000097567:Pleuromutilins
chemical_list: D000588:Amines; D004224:Diterpenes; D011083:Polycyclic Compounds; D000097567:Pleuromutilins