| Autor: |
Abdel-Maksoud MS; Medicinal & Pharmaceutical Chemistry Department, Pharmaceutical and Drug Industries Research Division, National Research Centre (NRC), Dokki, Giza 12622, Egypt. ph_ss@hotmail.com., El-Gamal MI; Department of Medicinal Chemistry, College of Pharmacy, University of Sharjah, Sharjah 27272, United Arab Emirates. drmelgamal2002@gmail.com.; Sharjah Institute for Medical Research, University of Sharjah, Sharjah 27272, United Arab Emirates. drmelgamal2002@gmail.com.; Department of Medicinal Chemistry, Faculty of Pharmacy, University of Mansoura, Mansoura 35516, Egypt. drmelgamal2002@gmail.com., Gamal El-Din MM; Medicinal & Pharmaceutical Chemistry Department, Pharmaceutical and Drug Industries Research Division, National Research Centre (NRC), Dokki, Giza 12622, Egypt. dr.m.g.eldin@hotmail.com., Choi Y; Department of Chemistry, Hanseo University, Seosan 31962, Korea. cossmoss@paran.com., Choi J; Department of Chemistry, Hanseo University, Seosan 31962, Korea. lovely1131@nate.com., Shin JS; Department of Pharmaceutical Biochemistry, College of Pharmacy, Kyung Hee University, Seoul 02792 Korea. jsshin@khu.ac.kr.; Department of Life and Nanopharmaceutical Science, College of Pharmacy, Kyung Hee University, Seoul 130-650, Korea. jsshin@khu.ac.kr., Kang SY; Department of Pharmaceutical Biochemistry, College of Pharmacy, Kyung Hee University, Seoul 02792 Korea. kang940818@naver.com.; Department of Life and Nanopharmaceutical Science, College of Pharmacy, Kyung Hee University, Seoul 130-650, Korea. kang940818@naver.com., Yoo KH; Department of Chemistry, Hanseo University, Seosan 31962, Korea. khyoo@kist.re.kr., Lee KT; Department of Pharmaceutical Biochemistry, College of Pharmacy, Kyung Hee University, Seoul 02792 Korea. ktlee@khu.ac.kr.; Department of Life and Nanopharmaceutical Science, College of Pharmacy, Kyung Hee University, Seoul 130-650, Korea. ktlee@khu.ac.kr., Baek D; Department of Chemistry, Hanseo University, Seosan 31962, Korea. djbaek@hanseo.ac.kr., Oh CH; Center for Biomaterials, Korea Institute of Science and Technology, Cheongryang, Seoul 130-650, Korea. choh@kist.re.kr.; Department of Biomolecular Science, University of Science and Technology, Daejeon, Yuseong-gu 34113, Korea. choh@kist.re.kr. |
| Abstrakt: |
This article describes the design, synthesis, and in vitro anti-inflammatory screening of new triarylpyrazole derivatives. A total of 34 new compounds were synthesized containing a terminal arylsulfonamide moiety and a different linker between the sulfonamide and pyridine ring at position 4 of the pyrazole ring. All the target compounds were tested for both cytotoxicity and nitric oxide (NO) production inhibition in lipopolysaccharide (LPS)-induced RAW 264.7 macrophages. Compounds 1b, 1d, 1g, 2a, and 2c showed the highest NO inhibition percentages and the lowest cytotoxic effect. The most potent derivatives were tested for their ability to inhibit prostaglandin E₂ (PGE₂) in LPS-induced RAW 264.7 macrophages. The IC 50 for nitric oxide inhibition, PGE₂ inhibition, and cell viability were determined. In addition, 1b, 1d, 1g, 2a, and 2c were tested for their inhibitory effect on LPS-induced inducible nitric oxide synthase (iNOS) and Cyclooxygenase 2 (COX-2) protein expression as well as iNOS enzymatic activity. |
