Synthesis and inhibitory effects of triarylpyrazoles on LPS-induced NO and PGE(2) productions in RAW 264.7 macrophages
- Synthesis and inhibitory effects of triarylpyrazoles on LPS-induced NO and PGE(2) productions in RAW 264.7 macrophages
- 유경호; 오창현; Byung-Jun Park; Mohammed I. El-Gamal; Woo-Suck Lee; Ji-Sun Shin; Kyung-Tae Lee
- Issue Date
- Medicinal chemistry research
- VOL 26, NO 9-2171
- The inhibition of nitric oxide and prostaglandin E2 productions is a very interesting research topic in the field of anti-inflammatory drug development. In the current study, a new series of 1,3,4-triarylpyrazole derivatives was synthesized and evaluated for their capabilities to inhibit nitric oxide and prostaglandin E2 productions in lipopolysaccharide-induced RAW 264.7 macrophages. Among all the target analogs, the diarylurea hydroxyl compounds 1f and 1h possessing phenyl and 3-(trifluoromethyl)phenyl terminal moiety, respectively, showed the highest inhibitory effect on the production of prostaglandin E2. Both compounds exerted equal activity to the reference compound NS-398 at 3  µ M concentration. This effect was due to inhibition cyclooxygenase-2 enzyme activity not inhibition of cyclooxygenase-2 protein expression. The IC50 value of compound 1f against lipopolysaccharide-induced prostaglandin E2 production in the macrophages was 1.12  μM. In addition, compound 1j with urea linker, hydroxyl group, and 3,5-bis(trifluoromethyl)phenyl terminal ring was the strongest nitric oxide inhibitor. Western blot study showed that it exerted that effect through inhibition of inducible nitric oxide synthase protein expression.
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