Pyrazolone methylamino piperidine derivatives as novel CCR3 antagonists

…, N Van Houtvin, M Van Thuyne, BJ van Keulen

Index: Pegurier, Cecile; Collart, Philippe; Danhaive, Pierre; Defays, Sabine; Gillard, Michel; Gilson, Frederic; Kogej, Thierry; Pasau, Patrick; Van Houtvin, Nathalie; Van Thuyne, Marc; van Keulen, BerendJan Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 15 p. 4228 - 4231

Full Text: HTML

Citation Number: 36

Abstract

The discovery and optimization of a novel class of potent CCR3 antagonists is described. Details of synthesis and SAR are given together with some ADME properties of selected compounds. An optimal balance between activities, physicochemical properties, and in vitro metabolic stability was reached by the proper choice of substituents.