Synthesis and structure-activity relationship of the first nonpeptidergic inverse agonists for the human cytomegalovirus encoded chemokine receptor US28

JW Hulshof, P Casarosa, WMPB Menge…

Index: Hulshof, Janneke W.; Casarosa, Paola; Menge, Wiro M. P. B.; Kuusisto, Leena M. S.; Van Der Goot, Henk; Smit, Martine J.; De Esch, Iwan J. P.; Leurs, Rob Journal of Medicinal Chemistry, 2005 , vol. 48, # 20 p. 6461 - 6471

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Citation Number: 32

Abstract

US28 is a human cytomegalovirus (HCMV) encoded G-protein-coupled receptor that signals in a constitutively active manner. Recently, we identified 1 {5-(4-(4-chlorophenyl)-4- hydroxypiperidin-1-yl)-2, 2-diphenylpentanenitrile} as the first reported nonpeptidergic inverse agonist for a viral-encoded chemokine receptor. Interestingly, this compound is able to partially inhibit the viral entry of HIV-1. In this study we describe the synthesis of 1 and ...