Synthesis and antibacterial activity of 3-O-acyl-6-O-carbamoyl erythromycin A derivatives.
A series of 3-O-acyl-6-O-carbamoyl erythromycin A derivatives has been synthesized. Several functional groups were identified as the optimal C3-substituents, and the best compounds in this series possess potent in vitro antibacterial activity against erythromycin-susceptible and erythromycin-resistant bacteria.
Zhu
Bin
B
Drug Discovery, Johnson & Johnson Pharmaceutical Research and Development, L.L.C. 1000 Route 202, PO Box 300, Raritan, NJ 08869, USA. bzhu@prdus.jnj.com
Marinelli
Brett A
BA
Abbanat
Darren
D
Foleno
Barbara D
BD
Henninger
Todd C
TC
Bush
Karen
K
Macielag
Mark J
MJ
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects*; D004917:Erythromycin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D048628:Ketolides / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D008968:Molecular Conformation; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D048628:Ketolides; D004917:Erythromycin; C106791:telithromycin