Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1

Ø Rist, M Grimstrup, JM Receveur, TM Frimurer…

文献索引：Rist, ystein; Grimstrup, Marie; Receveur, Jean-Marie; Frimurer, Thomas M.; Ulven, Trond; Kostenis, Evi; Hoegberg, Thomas Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 3 p. 1177 - 1180

全文：HTML全文

被引用次数: 7

摘要

Structure–activity relationships of three related series of 4-phenylthiazol-5-ylacetic acids, derived from two hits emanating from a focused library obtained by in silico screening, have been explored as CRTH2 (chemoattractant receptor-homologous molecule expressed on Th2 cells) antagonists. Several compounds with double digit nanomolar binding affinity and full antagonistic efficacy for human CRTH2 receptor were obtained in all subclasses. The ...