Synthesis and in silico investigation of thiazoles bearing pyrazoles derivatives as anti-inflammatory agents |
| |
| Affiliation: | 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 Chemistry, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad 431004, India;2. Combi Chem-Bio Resource Centre, CSIR-National Chemical Laboratory, Pune 411008, India;1. Department of Chemistry, Faculty of Science, University of Cairo, Giza 12613, Egypt;2. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Al-Azhar University, Cairo 11884, Egypt;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 Chemistry, Jamia Millia Islamia (A Central University), Jamia Nagar, New Delhi 110025, India;2. School of Biotechnology, Jawaharlal Nehru University, New Delhi 110067, India;3. Special Centre for Molecular Medicine, Jawaharlal Nehru University, New Delhi 110067, India;4. Department of Chemistry, University of Delhi, Delhi 110007, India |
| |
| Abstract: | Searching novel, safe and effective anti-inflammatory agents has remained an evolving research enquiry in the mainstream of inflammatory disorders. In the present investigation series of thiazoles bearing pyrazole as a possible pharmacophore were synthesized and assessed for their anti inflammatory activity using in vitro and in vivo methods. In order to decipher the possible anti-inflammatory mechanism of action of the synthesized compounds, cyclooxygenase I and II (COX-I and COX-II) inhibition assays were also carried out. The results obtained clearly focus the significance of compounds 5d, 5h and 5i as selective COX-II inhibitors. Moreover, compound 5h was also identified as a lead molecule for inhibition of the carrageenin induced rat paw edema in animal model studies. Molecular docking results revealed significant interactions of the test compounds with the active site of COX-II, which perhaps can be explored for design and development of novel COX-II selective anti-inflammatory agents. |
| |
| Keywords: | Anti-inflammatory COX Pyrazole Thiazole |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
