Park, Byung-Jun El-Gamal, Mohammed I. Lee, Woo-Suck Shin, Ji-Sun Yoo, Kyung Ho Lee, Kyung-Tae Oh, Chang-Hyun 2024-01-20T00:33:48Z 2024-01-20T00:33:48Z 2021-09-05 2017-09 1054-2523 https://pubs.kist.re.kr/handle/201004/122339 The inhibition of nitric oxide and prostaglandin E-2 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 E-2 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 E-2. Both compounds exerted equal activity to the reference compound NS-398 at 3 mu 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 mu M. 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. English SPRINGER BIRKHAUSER NF-KAPPA-B NITRIC-OXIDE DERIVATIVES PYRAZOLE CYCLOOXYGENASE-2 CANCER AGENTS RISK Synthesis and inhibitory effects of triarylpyrazoles on LPS-induced NO and PGE(2) productions in RAW 264.7 macrophages Article 10.1007/s00044-017-1923-9 1 MEDICINAL CHEMISTRY RESEARCH, v.26, no.9, pp.2161 - 2171 MEDICINAL CHEMISTRY RESEARCH 26 9 2161 2171 scie scopus 000406602000031 2-s2.0-85019743389 Chemistry, Medicinal Pharmacology & Pharmacy Article NF-KAPPA-B NITRIC-OXIDE DERIVATIVES PYRAZOLE CYCLOOXYGENASE-2 CANCER AGENTS RISK Anti-inflammatory Diarylurea Nitric oxide PGE(2) Pyrazole