CCR5 receptor antagonists: discovery and SAR study of guanylhydrazone derivatives

…, D Davey, L Dunning, W Lee, SF Lu, J Onuffer…

Index: Wei, Robert G.; Arnaiz, Damian O.; Chou, Yuo-Ling; Davey, Dave; Dunning, Laura; Lee, Wheeseong; Lu, Shou-Fu; Onuffer, James; Ye, Bin; Phillips, Gary Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 1 p. 231 - 234

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Citation Number: 18

Abstract

High throughput screening (HTS) led to the identification of the guanylhydrazone of 2-(4- chlorobenzyloxy)-5-bromobenzaldehyde as a CCR5 receptor antagonist. Initial modifications of the guanylhydrazone series indicated that substitution of the benzyl group at the para-position was well tolerated. Substitution at the 5-position of the central phenyl ring was critical for potency. Replacement of the guanylhydrazone group led to the discovery ...