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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 
Citation
 Chemical Biology & Drug Design, Vol.80(3) : 388~397, 2012 
Journal Title
 Chemical Biology & Drug Design 
ISSN
 1747-0277 
Issue Date
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://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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Link
 http://onlinelibrary.wiley.com/doi/10.1111/j.1747-0285.2012.01404.x/abstract
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