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
디팍이선희서선희남길수강순방배애님김은경오태권조상래금교창
Keywords
Antibacterial agents; Drug Design; drug discovery; Mycobacterium tuberclosis; oxazolidinone
Issue Date
2012-09
Publisher
Chemical biology & drug design
Citation
VOL 80, NO 3, 388-397
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://pubs.kist.re.kr/handle/201004/43742
ISSN
17470277
Appears in Collections:
KIST Publication > Article
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