Molecular design, synthesis and biological evaluation of cyclic imides bearing benzenesulfonamide fragment as potential COX-2 inhibitors. Part 2

IA Al-Suwaidan, AM Alanazi, AS El-Azab…

Index: Al-Suwaidan, Ibrahim A.; Alanazi, Amer M.; El-Azab, Adel S.; Al-Obaid, Abdulrahman M.; Eltahir, Kamal E.H.; Maarouf, Azza R.; Abu El-Enin, Mohamed A.; Abdel-Aziz, Alaa A.-M. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 9 p. 2601 - 2605

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Citation Number: 13

Abstract

A group of cyclic imides (1–10) was designed for evaluation as a selective COX-2 inhibitors and investigated in vivo for their anti-inflammatory activity. Compounds 6a, 6b, 8a, 8b, 9a, 9b, 10a and 10b were proved to be potent COX-2 inhibitors with IC50 range of 0.1–4.0 μM. In vitro COX-1/COX-2 inhibition structure–activity studies identified compound 8a as a highly potent (IC50= 0.1 μM), and an extremely selective [COX-2 (SI)> 1000] comparable to ...