✦ LIBER ✦

Design, synthesis and activity of benzothiazole-based inhibitors of NO production in LPS-activated macrophages

✍ Scribed by Guo Hua Jin; Hua Li; Semi An; Jae-Ha Ryu; Raok Jeon

Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 902 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.08.112

No coin nor oath required. For personal study only.

✦ Synopsis

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 lM 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-jB inactivation.

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