Synthesis and antibacterial activity of novel C12 vinyl ketolides

…, L Barker, K Huh, M Langhorne, R Shawar…

Index: Burger, Matthew T.; Lin, Xiaodong; Chu, Daniel T.; Hiebert, Christy; Rico, Alice C.; Seid, Mehran; Carroll, Georgia L.; Barker, Lynn; Huh, Kay; Langhorne, Mike; Shawar, Ribhi; Kidney, Jolene; Young, Kelly; Anderson, Scott; Desai, Manoj C.; Plattner, Jacob J. Journal of Medicinal Chemistry, 2006 , vol. 49, # 5 p. 1730 - 1743

Full Text: HTML

Citation Number: 23

Abstract

A novel series of C12 vinyl erythromycin derivatives have been discovered which exhibit in vitro and in vivo potency against key respiratory pathogens. The C12 modification involves replacing the natural C12 methyl group in the erythromycin core with a vinyl group via chemical synthesis. From the C12 vinyl macrolide core, a series of C12 vinyl ketolides was prepared. Several compounds were found to be potent against macrolide-sensitive and- ...