title: Synthesis and antibacterial activities of new piperidine substituted (5R)-[1,2,3]triazolylmethyl and (5R)-[(4-F-[1,2,3]triazolyl)methyl] oxazolidinones.
abstract: A novel series of 5(R)-[1,2,3]triazolylmethyl and (5R)-[(4-F-[1,2,3]triazolyl)methyl]oxazolidinones having various piperidine group were synthesized and evaluated antibacterial activity against clinically isolated resistant strains of Gram-positive and Gram-negative bacteria. The compound 12a having exo-cyanoethylidene group in the 4-position of piperidine ring was found to be two to threefold more potent than the linezolid against penicillin-resistant Staphylococcus pneumonia and Staphylococcus agalactiae, and also exhibited reduced MAO-B inhibitory activity.
authors: Center for Neuro-Medicine, Brain Science Institute, Korea Institutes of Science and Technology, Hwarangno 14-gil 5, Seoungbuk-gu, Seoul 136-791, South Korea.
authors: Hyo-Nim
authors: HN
authors: Shin
authors: Seon Hee
authors: SH
authors: Seo
authors: Hyunah
authors: H
authors: Choo
authors: Gyochang
authors: G
authors: Kuem
authors: Kyung Il
authors: KI
authors: Choi
authors: Ghilsoo
authors: G
authors: Nam
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D023303:Oxazolidinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D010880:Piperidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011023:Pneumonia, Staphylococcal / Q000188:drug therapy / Q000382:microbiology; D013210:Staphylococcus / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D023303:Oxazolidinones; D010880:Piperidines