Novel 2-(2-(benzylthio)-1H-benzo [d] imidazol-1-yl) acetic acids: discovery and hit-to-lead evolution of a selective CRTh2 receptor antagonist chemotype

…, MA Riederer, O Peter, X Leroy, A Valdenaire…

Index: Pothier, Julien; Riederer, Markus A.; Peter, Oliver; Leroy, Xavier; Valdenaire, Anja; Gnerre, Carmela; Fretz, Heinz Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 14 p. 4660 - 4664

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Citation Number: 10

Abstract

Hit-to-lead evolution of 2-(2-((2-(4-chlorophenoxy) ethyl) thio)-1H-benzo [d] imidazol-1-yl) acetic acid (1), discovered in a high-throughput screening campaign as a novel chemotype of CRTh2 receptor antagonist, is presented. SAR development as well as in vitro and in vivo DMPK properties of selected representatives of substituted 2-(2-(benzylthio)-1H-benzo [d] imidazol-1-yl) acetic acids are discussed.