Synthesis and In Vitro Antibacterial Activity of Novel 3-Azabicyclo[3.3.0]octanyl Oxazolidinones
- Synthesis and In Vitro Antibacterial Activity of Novel 3-Azabicyclo[3.3.0]octanyl Oxazolidinones
- 디팍; 이선희; 서선희; 남길수; 강순방; 배애님; 김은경; 오태권; 조상래; 금교창
- Antibacterial agents; Drug Design; drug discovery; Mycobacterium tuberclosis; oxazolidinone
- Issue Date
- Chemical biology & drug design
- VOL 80, NO 3, 388-397
- 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.
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