Thieno[3,2-b]thiophene-2-carboxylic acid derivatives as GPR35 agonists
Thieno[3,2-b]thiophene-2-carboxylic acid derivatives as GPR35 agonists
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DOI：
10.1016/j.bmcl.2012.04.057
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发表时间：
2012-06-15
影响因子：
2.7
通讯作者：
Fang, Ye
中科院分区：
文献类型：
--
作者：
Deng, Huayun;Hu, Jieyu;Fang, Ye
报道了一系列硫代[3，2-b]噻吩基-2-羧酸衍生物对GPR35的激动剂活性的优化。化合物被优化以实现β-芳香素偏向激动剂，以开发可能有助于阐明GPR35生物学和生理学的探针分子。化合物13被鉴定为最有效的GPR35激动剂，化合物30和36表现出最高的诱导β-arrestin易位的效果。(C)2012爱思唯尔有限公司。保留所有权利。
The optimization of a series of thieno[3,2-b]thiophene-2-carboxylic acid derivatives for agonist activity against the GPR35 is reported. Compounds were optimized to achieve beta-arrestin-biased agonism for developing probe molecules that may be useful for elucidating the biology and physiology of GPR35. Compound 13 was identified to the most potent GPR35 agonist, and compounds 30 and 36 exhibited the highest efficacy to cause beta-arrestin translocation. (C) 2012 Elsevier Ltd. All rights reserved.