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

[摘要]：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 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-kappa B inactivation. (C) 2010 Elsevier Ltd. All rights reserved.

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