European journal of medicinal chemistry

Synthesis, anti-inflammatory activity and COX-1/COX-2 inhibition of novel substituted cyclic imides. Part 1: Molecular docking study

AM Alaa, KEH ElTahir, YA Asiri

文献索引：Abdel-Aziz, Alaa A.-M.; Eltahir, Kamal E.H.; Asiri, Yousif A. European Journal of Medicinal Chemistry, 2011 , vol. 46, # 5 p. 1648 - 1655

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被引用次数: 48

摘要

A group of cyclic imides (1–13) was designed for evaluation as selective COX-2 inhibitors and investigated in vivo for their anti-inflammatory activities using carrageenan-induced rat paw edema model. Compounds 5b, 6b, 11b, 11c, 12b and 12c were proved to be potent COX-2 inhibitors with IC50 range of 0.1–1.0 μM. In vitro COX-1/COX-2 inhibition structure– activity studies identified compound 5b as a highly potent (IC50= 0.1 μM), and an ...