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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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18초록
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
Benzothiazole; Nitric oxide; NOS; Inhibitor; NITRIC-OXIDE SYNTHASE; DIMERIZATION INHIBITORS; SELECTIVE INHIBITORS; IN-VITRO; POTENT; ISOFORMS; INACTIVATION; MECHANISM; ENZYME
- 제목
- Design, synthesis and activity of benzothiazole-based inhibitors of NO production in LPS-activated macrophages
- 저자
- Jin, Guo Hua; Li, Hua; An, Semi; Ryu, Jae-Ha; Jeon, Raok
- 발행일
- 2010-11-01
- 유형
- Article
- 권
- 20
- 호
- 21
- 페이지
- 6199 ~ 6202