title: Pleuromutilin derivatives having a purine ring. Part 2: influence of the central spacer on the antibacterial activity against Gram-positive pathogens.
abstract: Structural modification of the 4-piperidinethio moiety, as a spacer of the first pleuromutilin analogues 2A and 2B having a purine ring, led to discovery of the novel pleuromutilin derivatives 14B and 17B. These compounds with good solubility in water showed promising in vitro antibacterial activity against various Gram-positive bacteria including MRSA, PRSP, and VRE and have potent in vivo efficacy.
authors.affiliation: Chemistry Research Laboratories, Dainippon Sumitomo Pharma Co, Ltd, Enoki, Suita, Japan.
authors.forename: Yoshimi
authors.initials: Y
authors.lastname: Hirokawa
authors.forename: Hironori
authors.initials: H
authors.lastname: Kinoshita
authors.forename: Tomoyuki
authors.initials: T
authors.lastname: Tanaka
authors.forename: Takanori
authors.initials: T
authors.lastname: Nakamura
authors.forename: Koichi
authors.initials: K
authors.lastname: Fujimoto
authors.forename: Shigeki
authors.initials: S
authors.lastname: Kashimoto
authors.forename: Tsuyoshi
authors.initials: T
authors.lastname: Kojima
authors.forename: Shiro
authors.initials: S
authors.lastname: Kato
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology; D004224:Diterpenes / Q000737:chemistry; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D011083:Polycyclic Compounds; D011687:Purines / Q000737:chemistry*; D012995:Solubility; D013329:Structure-Activity Relationship; D000097567:Pleuromutilins
chemical_list: D000900:Anti-Bacterial Agents; D004224:Diterpenes; D011083:Polycyclic Compounds; D011687:Purines; D000097567:Pleuromutilins; C030985:purine