COX-1/COX-2 inhibition assays and histopathological study of the new designed anti-inflammatory agent with a pyrazolopyrimidine core |
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| Institution: | 1. Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Beni-Suef University, Beni-Suef 62514, Egypt;2. Department of Pathology, Faculty of Veterinary Medicine, Beni-suef University, 62511, Egypt;1. Research and Development Centre, Bharathiar University, Coimbatore 641046, India;2. Department of Biotechnology, School of Bio-Sciences and Technology, VIT University, Vellore 632014, India;3. PG & Research Department of Chemistry, Government Arts College, Coimbatore 641018, Tamil Nadu, India;1. Department of Chemical Technology, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad 431004, Maharashtra, India;2. School of Life Sciences, University of Hyderabad, Hyderabad, India;1. College of Pharmacy, Al Ain University of Science and Technology, Al Ain, United Arab Emirates;2. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt;3. Department of Veterinary Medicine, College of Agricultural and Veterinary Medicine, Qassim University, Saudi Arabia;4. Department of Pharmacology, Faculty of Veterinary Medicine, Alexandria University, Alexandria, Egypt;5. Department of Chemistry, University of Prince Edward Island, Charlottetown, Prince Edward Island C1A 4P3, Canada;1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Alexandria University, Alexandria 21521, Egypt;2. Department of Medical Biochemistry, Faculty of Medicine, Alexandria University, Alexandria, Egypt;1. Al-Azhar University, Faculty of Pharmacy, Pharmaceutical Organic Chemistry Department, Assiut 71524, Egypt;2. Cairo University, Faculty of Pharmacy, Pharmaceutical Organic Chemistry Department, Cairo 11562, Egypt;3. South Dakota State University, Faculty of Science, Chemistry Department, Brookings, SD 57007, USA |
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| Abstract: | Four pyrazolopyrimidine series were prepared with a substitution at position- 4 by Schiff base, triazole, oxadiazole and pyrazole moieties (7a-f, 8a,b, 9a-f, 10a,b and 13a,b), respectively. All the synthesized compounds were evaluated in vitro against COX-2 and in vivo against carrageenan-induced rat paw edema as anti-inflammatory agents. Regarding the anti-inflammatory activity (AI) compounds 7c, 7f, 8a, and 9a showed higher activity with respect to celecoxib. Compounds 9a, 7d, and 7f were closely selective to celecoxib. Also, 7c and 7d were safer than indomethacin and similar to celecoxib as resulted from the histopathological study. In addition, the docking study that showed the binding mode of prominent pyrazolopyrimidine compounds inside the COX-2 receptor. Formation of unexpected pyrazole 13a and 13b was briefly discussed using 2D NMR. |
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| Keywords: | Anti-inflammatory Celecoxib COX-2 inhibitors |
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