title: Synthesis of 2-methyl 16-membered macrolide derived from tylosin.
abstract: To improve the metabolic stability of a 16-membered macrolide, 2-methylated derivatives of desmycosin were synthesized. Among these derivatives, 2beta-methyldesmycosin retained antibacterial activity and showed improved stability in rat serum compared to desmycosin.
authors.affiliation: Medicinal Research Laboratories, Taisho Pharmaceutical Co., Ltd., 1-403, Yoshinocho, Kita-ku, Saitama-shi, Saitama 331-9530, Japan. yuichi.terui@po.rd.taisho.co.jp
authors.forename: Yuichi
authors.initials: Y
authors.lastname: Terui
authors.forename: Kenji
authors.initials: K
authors.lastname: Kinoshita
authors.forename: Yoshie
authors.initials: Y
authors.lastname: Kaneda
authors.forename: Toshi
authors.initials: T
authors.lastname: Akashi
authors.forename: Takuya
authors.initials: T
authors.lastname: Hamaguchi
authors.forename: Akira
authors.initials: A
authors.lastname: Kawashima
mesh_terms: D000818:Animals; D043182:Carboxylesterase / Q000378:metabolism; D006193:Haemophilus influenzae / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D051381:Rats; D044967:Serum / Q000201:enzymology; D013296:Streptococcus pneumoniae / Q000187:drug effects; D015645:Tylosin / Q000031:analogs & derivatives* / Q000096:biosynthesis / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology
chemical_list: C052318:tylosin B; D043182:Carboxylesterase; D015645:Tylosin