Synthesis of 3,6-bicyclolides: a novel class of macrolide antibiotics.
The synthesis of 3,6-bicyclolides from erythromycin A oxime is described. This novel class of bridged bicyclic macrolides demonstrates potent in vitro and in vivo activities against a broad spectrum of bacteria including resistant respiratory tract pathogens.
Gai
Yonghua
Y
Enanta Pharmaceuticals, Inc., 500 Arsenal Street, Watertown, MA 02472, USA.
Tang
Datong
D
Xu
Guoyou
G
Chen
Zhigang
Z
Polemeropoulos
Alexander
A
Wang
Zhe
Z
Or
Yat Sun
YS
D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D018360:Crystallography, X-Ray / Q000379:methods; D015195:Drug Design; D018432:Drug Resistance, Multiple; D006801:Humans; D018942:Macrolides / Q000138:chemical synthesis* / Q000737:chemistry* / Q000145:classification*; D051379:Mice; D008826:Microbial Sensitivity Tests; D008956:Models, Chemical; D008968:Molecular Conformation; D012137:Respiratory System / Q000382:microbiology
D000900:Anti-Bacterial Agents; D018942:Macrolides