Design, synthesis and activity of benzothiazole-based inhibitors of NO production in LPS-activated macrophages
  • Jin, Guo Hua
  • Li, Hua
  • An, Semi
  • Ryu, Jae-Ha
  • Jeon, Raok
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초록

Series of benzothiazoles were synthesized and evaluated their inhibitory activities for NO production in lipopolysaccharide-activated macrophages. The most potent compound was the indole-containing benzothiazole 3c with 4.18 mu M of IC(50). The mechanistic study suggested that benzothiazoles inhibited NO production by the suppression of iNOS protein and mRNA expression. They also suppressed the expression of COX-2 through the NF-kappa B inactivation. (C) 2010 Elsevier Ltd. All rights reserved.

키워드

BenzothiazoleNitric oxideNOSInhibitorNITRIC-OXIDE SYNTHASEDIMERIZATION INHIBITORSSELECTIVE INHIBITORSIN-VITROPOTENTISOFORMSINACTIVATIONMECHANISMENZYME
제목
Design, synthesis and activity of benzothiazole-based inhibitors of NO production in LPS-activated macrophages
저자
Jin, Guo HuaLi, HuaAn, SemiRyu, Jae-HaJeon, Raok
DOI
10.1016/j.bmcl.2010.08.112
발행일
2010-11-01
유형
Article
저널명
Bioorganic and Medicinal Chemistry Letters
20
21
페이지
6199 ~ 6202