COX-1/COX-2 inhibition assays and histopathological study of the new designed anti-inflammatory agent with a pyrazolopyrimidine core

被引：33
作者：
Abdelall, Eman K. A. [1 ]
Lamie, Phoebe F. [1 ]
Ahmed, Amira K. M. [1 ]
El-Nahass, El-Shaymaa [2 ]
机构：
[1] Beni Suef Univ, Dept Pharmaceut Organ Chem, Fac Pharm, Bani Suwayf 62514, Egypt
[2] Beni Suef Univ, Fac Vet Med, Dept Pathol, Bani Suwayf 62511, Egypt
来源：
BIOORGANIC CHEMISTRY | 2019年 / 86卷
关键词：
Anti-inflammatory; Celecoxib; COX-2; inhibitors; Pyrazolo[3,4-d] pyrimidine; SO2Me pharamacophores; PHARMACOLOGICAL EVALUATION; BIOLOGICAL EVALUATION; PYRAZOLE CYCLIZATION; DERIVATIVES; CYCLOOXYGENASE-2; PYRIMIDINE; COX-2;
D O I：
10.1016/j.bioorg.2019.01.031
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
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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页码：235 / 253
页数：19
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