121st General Meeting of the KCS

Type Poster Presentation
Area Medicinal Chemistry
Room No. Event Hall
Time 4월 19일 (목요일) 11:00~12:30
Code MEDI.P-592
Subject Anti-inflammatory activity of novel triaryl pyrazole derivatives possessing sulfonamide moiety
Authors Chang Hyun Oh*, Mohammed Abdel maksoud1, Eslam M. H. Ali1, Usama Ammar1, Kyung Ho Yoo2, Mohammed EL-Gamal3
Center for Bio Materials, Korea Institute of Science and Technology, Korea
1University of Science & Technology, Korea
2Chemical Kinomics Research Center, Korea Institute of Science and Technology, Korea
3Department of Medicinal Chemistry, University of Mansoura, Egypt
Abstract In current study, a new series of triaryl pyrazole derivatives was synthesized and evaluated for their anti-inflammatory activity. The new compounds were tested for their effect on nitric oxide production in LPS-induced RAW 264.7 macrophages. Compounds KIST 301, KIST 305, KIST 306, KIST 320 and KIST 322 were the most potent one with IC50s 8.23, 7.90, 8.55, 8.04 and 6.68 μM respectively. The most potent compounds were further investigated for PGE2 production, and COX-1/2 activity in LPS-induced RAW 264.7 macrophages. KIST 306 showed the highest activity against PGE2 production. On the other hand none of the tested compounds exhibited activity against COX1/2.
E-mail choh@kist.re.kr