期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 14, 页码 4660-4664出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.05.087
关键词
CRTh2; DP2; Prostaglandin; Asthma; Rhinitis
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. (C) 2012 Elsevier Ltd. All rights reserved.
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