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Synthesis and in vitro antibacterial activity of novel 3-azabicyclo[3.3.0]octanyl oxazolidinones.

Title
Synthesis and in vitro antibacterial activity of novel 3-azabicyclo[3.3.0]octanyl oxazolidinones.
Authors
Deepak Bhattarai;Sun H. Lee;Gyochang Keum;Sang-Nae Cho;Taegwon Oh;Eunice E. Kim;Ae N. Pae;Soon B. Kang;Ghilsoo Nam;Seon H. Seo
Issue Date
2012
Journal Title
Chemical Biology & Drug Design
ISSN
1747-0277
Citation
Chemical Biology & Drug Design, Vol.80(3) : 388~397, 2012
Abstract
We synthesized a series of oxazolidinone-type antibacterials in which morpholine C-ring of linezolid has been modified by substituted 3-azabicyclo[3.3.0]octanyl rings. Acetamide or 1,2,3-triazole heterocycle was used as C-5 side chain of oxazolidinone. The resulting series of compounds was then screened in vitro against panel of susceptible and resistant Gram-positive, Gram-negative bacteria, and Mycobacterium tuberculosis (Mtb). Several analogs in this series exhibited potent in vitro antibacterial activity comparable or superior to linezolid against the tested bacteria. Compounds 10a, 10b, 11a, and 15a displayed highly potent activity against M. tuberculosis. Selected compound 10b showed good human microsomal stability and CYP-profile, and showed low activity against hERG channel.
URI
http://onlinelibrary.wiley.com/doi/10.1111/j.1747-0285.2012.01404.x/abstract

http://ir.ymlib.yonsei.ac.kr/handle/22282913/89935
DOI
10.1111/j.1747-0285.2012.01404.x
Appears in Collections:
1. 연구논문 > 1. College of Medicine > Yonsei Biomedical Research Center
1. 연구논문 > 1. College of Medicine > Dept. of Microbiology
Yonsei Authors
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