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

GH Jin, H Li, S An, JH Ryu, R Jeon

Index: Jin, Guo Hua; Li, Hua; An, Semi; Ryu, Jae-Ha; Jeon, Raok Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 21 p. 6199 - 6202

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Citation Number: 10

Abstract

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 μM of IC50. 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-κB ...