1, 2-Diarylpyrroles as potent and selective inhibitors of cyclooxygenase-2

…, AW Veenhuizen, JL Currie, K Seibert…

Index: Khanna, Ish K.; Weier, Richard M.; Yu, Yi; Collins, Paul W.; Miyashiro, Julie M.; Koboldt, Carol M.; Veenhuizen, Amy W.; Currie, Jerry L.; Seibert, Karen; Isakson, Peter C. Journal of Medicinal Chemistry, 1997 , vol. 40, # 11 p. 1619 - 1633

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Citation Number: 190

Abstract

Series of 1, 2-diarylpyrroles has been synthesized and found to contain very potent and selective inhibitors of the human cyclooxygenase-2 (COX-2) enzyme. The paper describes short and practical syntheses of the target molecules utilizing the Paal-Knorr reaction. Electrophilic substitution on 1 proceeds in a regioselective fashion, and the method was used to generate a number of tetrasubstituted pyrroles. Detailed SAR on the series has ...