Synthesis and antibacterial activities of new piperidine substituted (5R)-[1,2,3]triazolylmethyl and (5R)-[(4-F-[1,2,3]triazolyl)methyl] oxazolidinones |
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| Authors: | Hyo-Nim Shin Seon Hee Seo Hyunah Choo Gyochang Kuem Kyung Il Choi Ghilsoo Nam |
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| Affiliation: | Center for Neuro-Medicine, Brain Science Institute, Korea Institutes of Science and Technology (KIST), Hwarangno 14-gil 5, Seoungbuk-gu, Seoul 136-791, South Korea |
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| 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. |
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