Synthesis,anti-inflammatory,analgesic, COX-1/2 inhibition activities and molecular docking study of pyrazoline derivatives |
| |
| Affiliation: | 1. Department of Medicinal Chemistry, Faculty of Pharmacy, University of Mansoura, Mansoura 35516, Egypt;2. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Delta University for Science and Technology, Gamasa City, Egypt;3. Department of Pharmacology, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia;4. Department of Pharmacology, Faculty of Pharmacy, University of Mansourua, Mansoura 35516, Egypt;5. Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia;1. Department of Obstetrics and Gynecology, Second Affiliated Hospital of Southeast University, Nanjing 210003, China;2. Department of Obstetrics and Gynecology, Huai’an Maternal and Child Health Hospital, 223002, China;3. Department of Obstetrics and Gynecology, Affiliated Hospital of Xuzhou Medical College, Xuzhou 221006, China;1. Heterocyclic Compounds Research Group, Department of Chemistry, Universidad del Valle, A. A. 25360 Cali, Colombia;2. PECET-SIU, Universidad de Antioquia, PO Box 1226, Medellín, Colombia;3. Department of Inorganic and Organic Chemistry, Universidad de Jaén, 23071 Jaén, Spain;1. Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, Egypt;2. Pharmacology Department, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, Egypt;1. School of Chemical Sciences, Swami Ramanand Teerth Marathwada University, Nanded, MH 431606, India;2. School of Life Sciences, Swami Ramanand Teerth Marathwada University, Nanded, MH 431606, India;1. Department of Biochemistry and Molecular Biology, Thomas Jefferson University, Philadelphia, PA 19107, USA;2. Institute of Biomembranes and Bioenergetics, National Research Council, Via Amendola 165/A, 70125 Bari, Italy;3. Department of Pharmacy - Pharmaceutical Sciences, University of Bari “Aldo Moro”, Via E. Orabona 4, 70125 Bari, Italy;4. Department of Scienze Chimiche, Università di Catania, Viale Andrea Doria 6, 95125 Catania, Italy;5. Department of Pharmaceutical Sciences, College of Pharmacy, Thomas Jefferson University, Philadelphia, PA 19107, USA;6. Department of Biological Chemistry, University of Michigan, Ann Arbor, MI 48109, USA |
| |
| Abstract: | Design, synthesis and pharmacological activities of a group of 1,3,5-trisubstituted pyrazolines were reported. The chemical structures of the synthesized compounds have been assigned on the basis of IR, MS, 1H NMR, and 13C NMR spectral analyses. The synthesized 1,3,5-trisubstituted pyrazoline derivatives were evaluated in vivo for anti-inflammatory, analgesic activities and in vitro for COX-1/2 inhibition assay. Among the tested compounds, derivatives 4h, 6e, 7a, 7e, and 9 showed more potent anti-inflammatory and analgesic activities than the reference drug celecoxib. On the basis of their higher activities in the in vivo studies compared with celecoxib, the five compounds 4h, 6e, 7a, 7e and 9 were selected to test their inhibitory activities against ovine COX-1/2 using an in vitro cyclooxygenase inhibition assay. Docking study of compounds 7a, 7e and 9 into the COX-2 binding site revealed a similar binding mode to SC-558, a selective COX-2 inhibitor. |
| |
| Keywords: | Pyrazoline derivatives Anti-inflammatory activity Selective COX-2 inhibition Molecular docking study |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
