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Bioorg Med Chem Lett. 2013 Mar 1;23(5):1193-6. doi: 10.1016/j.bmcl.2013.01.033. Epub 2013 Jan 16.

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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1
Center for Neuro-Medicine, Brain Science Institute, Korea Institutes of Science and Technology, Hwarangno 14-gil 5, Seoungbuk-gu, Seoul 136-791, South Korea.

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.

PMID:
23385213
DOI:
10.1016/j.bmcl.2013.01.033
[Indexed for MEDLINE]
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