Synthesis and antibacterial activity of 6-O-arylbutynyl ketolides with improved activity against some key erythromycin-resistant pathogens.
A series of novel 6-O-substituted homopropargyl ketolides was synthesized and evaluated against various erythromycin-resistant pathogens. Promising in vitro antibacterial activity was demonstrated for compounds bearing this structural motif.
Infectious Disease Research, Abbott Laboratories, D47P, AP52N, 200 Abbott Park Road, Abbott Park, Illinois 60064-6217, USA. robert.keyes@abbott.com
Robert F
RF
Keyes
Justin J
JJ
Carter
Erika E
EE
Englund
Melissa M
MM
Daly
Greg G
GG
Stone
Angela M
AM
Nilius
Zhenkun
Z
Ma
D000480:Alkynes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D024881:Drug Resistance, Bacterial; D004917:Erythromycin / Q000494:pharmacology*; D006193:Haemophilus influenzae / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D013210:Staphylococcus / Q000187:drug effects; D013329:Structure-Activity Relationship
D000480:Alkynes; D000900:Anti-Bacterial Agents; D004917:Erythromycin