Structure Activity of 3-Aryl-1, 3-diketo-Containing Compounds as HIV-1 Integrase Inhibitors 1

…, C Marchand, N Neamati, K Cowansage…

Index: Pais, Godwin C. G.; Zhang, Xuechun; Marchand, Christophe; Neamati, Nouri; Cowansage, Kiriana; Svarovskaia, Evguenia S.; Pathak, Vinay K.; Tang, Yun; Nicklaus, Marc; Pommier, Yves; Burke Jr., Terrence R. Journal of Medicinal Chemistry, 2002 , vol. 45, # 15 p. 3184 - 3194

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Citation Number: 200

Abstract

The 4-aryl-2-hydroxy-4-oxo-2-butenoic acids and their isosteric tetrazoles are among an emerging class of aryl β-diketo (ADK)-based agents which exhibit potent inhibition of HIV-1 integrase (IN)-catalyzed strand transfer (ST) processes, while having much reduced potencies against 3'-processing (3'-P) reactions. In the current study, L-708,906 (10e) and 5CITEP (13b), which are two examples of ADK inhibitors that have been reported by ...