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 β-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 β-arrestin translocation.

中文翻译：

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噻吩并[3,2 - b ]噻吩-2-羧酸衍生物作为GPR35激动剂

报道了针对硫代[3，2 - b ]噻吩-2-羧酸衍生物的一系列针对GPR35的激动剂活性的优化。优化化合物以实现β-arrestin偏置的激动作用，以开发可用于阐明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表现出引起β-arrestin易位的最高功效。