Article

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.

Actelion Pharmaceuticals Ltd, Gewerbestrasse, 16, CH-4123 Allschwil, Switzerland.
Bioorganic & medicinal chemistry letters (impact factor: 2.65). 06/2012; 22(14):4660-4. DOI:10.1016/j.bmcl.2012.05.087 pp.4660-4
Source: PubMed

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.

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Keywords

CRTh2 receptor antagonist
 
high-throughput screening campaign
 
Hit-to-lead evolution
 
representatives
 
vivo DMPK properties