Synthesis and antibacterial activity of oxazolidinones containing pyridine substituted with heteroaromatic ring.
A series of oxazolidinone derivatives, which morpholino group of linezolid was replaced with heteroaromatic ring substituted pyridine moiety, were newly synthesized, and their substituted effects on in vitro and in vivo antibacterial activities were evaluated against four problematic gram-positive strains including drug resistant strains and two gram-negative strains. Most compounds exhibited the enhanced in vitro activities with 4-16-fold and three compounds exerted more than 2-fold increased in vivo efficacies than linezolid.
Jo
Yeong Woo
YW
College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul 151-742, Korea.
Im
Weon Bin
WB
Rhee
Jae Keol
JK
Shim
Mi Ja
MJ
Kim
Won Bae
WB
Choi
Eung Chil
EC
D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D008826:Microbial Sensitivity Tests / Q000706:statistics & numerical data; D023303:Oxazolidinones / Q000138:chemical synthesis* / Q000494:pharmacology; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D023303:Oxazolidinones; D011725:Pyridines; C023666:pyridine