Design,synthesis and molecular docking of benzophenone conjugated with oxadiazole sulphur bridge pyrazole pharmacophores as anti inflammatory and analgesic agents |
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| Institution: | 1. Department of Chemistry, Yuvaraja’s College (Autonomous), University of Mysore, Mysuru, Karnataka, India;2. Department of Biochemistry, Farooqia Dental College, Mysuru, Karnataka, India;1. Department of Chemistry, Yuvaraja College, University of Mysore, Mysuru 570005, India;2. Center for the Study of Systems Biology, School of Biology, Georgia Institute of Technology, Atlanta, GA 30332, USA;3. Institution of Excellence, University of Mysore, Manasagangotri, Mysuru 570006, India;4. Department of Studies in Physics, University of Mysore, Manasagangotri, Mysuru 570006, India;5. Transplant Surgery Section, Rangos Research Center, University Of Pittsburgh, PA 15201, USA;1. Department of Chemistry, Faculty of Science, Jamia Hamdard (Hamdard University), New Delhi 110062, India;2. CSIR – Unit for Research and Development of Information Products (URDIP), Pune 411038, India;3. Department of Pharmacology, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), New Delhi 110062, India;1. Department of Physics, Fatima Mata National College, Kollam, Kerala, India;2. Department of Pharmaceutical Chemistry, Sinhgad Institute of Pharmacy, Narhe, Pune, University of Pune, Ganeshkhind, India;3. University of Novi Sad, Faculty of Sciences, Department of Physics, Trg D. Obradovi?a 4, 21000 Novi Sad, Serbia;4. University of Novi Sad, Faculty of Sciences, Department of Chemistry, Biochemistry and Environmental Protection, Trg D. Obradovi?a 3, 21000 Novi Sad, Serbia;5. Department of Chemistry, St. Berchmans College (Autonomous), Changanacherry, Kerala, India;6. Department of Chemistry, S.N. College, Kollam, Kerala, India;1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), New Delhi 110062, India;2. College of Pharmacy and Dentistry, Buraydah Private Colleges, Al-Qassim 31717, Saudi Arabia;3. School of Computational & Integrative Sciences, Jawaharlal Nehru University, New Delhi 110067, India;4. Department of Medicinal Chemistry, Maharishi Arvind College of Pharmacy Jaipur, Rajasthan 301 039, India;5. College of Clinical Pharmacy, University of Dammam, Dammam 31441, Saudi Arabia;6. Department of Pharmaceutical Sciences & Technology, Birla Institute of Technology, Mesra, Ranchi, Jharkhand 835 215, India;7. Department of Toxicology, Faculty of Science, Jamia Hamdard (Hamdard University), New Delhi 110062, India;1. Novosibirsk Institute of Organic Chemistry, Acad. Lavrentyev ave. 9, Novosibirsk 630090, Russia;2. The Federal Research Center Institute of Cytology and Genetics, Acad. Lavrentyev Ave., 10, 630090 Novosibirsk, Russia;3. Novosibirsk State University, Pirogov Street 2, 630090 Novosibirsk, Russia;4. Institute of Technology of Organic Chemistry, Faculty of Materials Science and Applied Chemistry, Riga Technical University, P. Valdena Str. 3, Riga LV-1048, Latvia;1. Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, N.P Marg, Matunga (East), Mumbai 400019, India;2. SVKM’s Dr. Bhanuben Nanavati College of Pharmacy, Gate No. 1, Mithibai College Campus, V.M. Road, Vile Parle (West), Mumbai 400056, India |
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| Abstract: | The prostaglandins (PG) a group of physiologically active lipid compounds having diverse hormone like effects are important mediators of the body’s response to pain and inflammation, and are formed from essential fatty acids found in cell membranes. This reaction is catalyzed by cyclooxygenase, a membrane associated enzyme occurring in two isoforms, COX-1 and COX-2. Nonsteroidal anti-inflammatory drugs (NSAIDs) act by inhibiting the activity of COX. In view of this, a series of novel benzophenones conjugated with oxadiazole sulphur bridge pyrazole moiety 8a-l were designed, synthesized, characterized and subsequently evaluated for anti-inflammatory and analgesic property. The investigation of novel analogues 8a-l for potential anti-inflammatory activity showed high levels of COX-1 and COX-2 inhibitory activity. Among the series, compound 8i with electron withdrawing fluoro group at the para position of the benzoyl ring of benzophenone was characterized by highest IC50 values for both COX-1 and COX-2 inhibition, which is comparable to the standard drug. Further, molecular docking studies have been performed for the potent compound. |
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| Keywords: | Benzophenone Pyrazole Inflammatory Analgesic Molecular docking studies |
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