title: Pleuromutilins. Part 1. The identification of novel mutilin 14-carbamates.
abstract: A novel series of mutilin 14-carbamates has been discovered as a result of structure-activity studies on the naturally occurring antibiotic pleuromutilin (1). In particular, the 4-methoxybenzoylcarbamate, SB-222734 (15o) displays potent antibacterial activity against a number of bacterial pathogens which are resistant to currently used agents and shows enhanced metabolic stability when compared to earlier pleuromutilin derivatives. Such derivatives therefore have the potential to provide a new class of antibacterial agents for human therapy which address the threat of bacterial resistance.
authors.affiliation: SmithKline Beecham Pharmaceuticals Research and Development, Discovery Chemistry Europe, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK
authors.forename: G
authors.initials: G
authors.lastname: Brooks
authors.forename: W
authors.initials: W
authors.lastname: Burgess
authors.forename: D
authors.initials: D
authors.lastname: Colthurst
authors.forename: J D
authors.initials: JD
authors.lastname: Hinks
authors.forename: E
authors.initials: E
authors.lastname: Hunt
authors.forename: M J
authors.initials: MJ
authors.lastname: Pearson
authors.forename: B
authors.initials: B
authors.lastname: Shea
authors.forename: A K
authors.initials: AK
authors.lastname: Takle
authors.forename: J M
authors.initials: JM
authors.lastname: Wilson
authors.forename: G
authors.initials: G
authors.lastname: Woodnutt
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D001685:Biological Factors / Q000737:chemistry / Q000494:pharmacology; D002219:Carbamates / Q000138:chemical synthesis / Q000494:pharmacology; D004224:Diterpenes / Q000138:chemical synthesis* / Q000494:pharmacology*; D004352:Drug Resistance, Microbial / Q000235:genetics / Q000502:physiology; D006193:Haemophilus influenzae / Q000187:drug effects*; D008826:Microbial Sensitivity Tests / Q000592:standards; D011083:Polycyclic Compounds; D013210:Staphylococcus / Q000187:drug effects*; D000097567:Pleuromutilins
chemical_list: D000900:Anti-Bacterial Agents; D001685:Biological Factors; D002219:Carbamates; D004224:Diterpenes; D011083:Polycyclic Compounds; D000097567:Pleuromutilins; C434329:mutilin 14-(N-(4-methoxybenzoyl))-carbamate; C014224:tiamulin