Discovery of DS-3801b, a non-macrolide GPR38 agonist with N-methylanilide structure,Bioorganic & Medicinal Chemistry Letters

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Discovery of DS-3801b, a non-macrolide GPR38 agonist with N-methylanilide structure
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2022-01-18 , DOI: 10.1016/j.bmcl.2022.128554
Narihiro Toda ₁ , Takeshi Shida ₁ , Rieko Takano ₁ , Takahiro Katagiri ₁ , Masakazu Hirouchi ₁ , Manabu Abe ₁ , Kaori Soma ₁ , Yasuhiro Nakagami ₁ , Mami Yamazaki ₁

Affiliation

Motilin is a 22-amino-acid gastrointestinal (GI) hormone and is involved in the regulation of GI motility through binding to GPR38, the motilin receptor which is expressed on smooth muscle cells in the GI tract. Therefore, GPR38 agonists are expected to be novel gastrointestinal prokinetic agents for the treatment of functional gastrointestinal disorders such as gastroparesis and chronic constipation. We identified a series of N-methylanilide derivatives as novel non-macrolide GPR38 agonists. Among them, 12 di-l-tartrate (DS-3801b) was selected as a clinical candidate for further evaluation.

中文翻译：

发现 DS-3801b，一种具有 N-甲基苯胺结构的非大环内酯 GPR38 激动剂

胃动素是一种 22 个氨基酸的胃肠 (GI) 激素，通过与 GPR38 结合参与调节 GI 运动，GPR38 是在胃肠道平滑肌细胞上表达的胃动素受体。因此，GPR38 激动剂有望成为治疗胃轻瘫和慢性便秘等功能性胃肠疾病的新型胃肠促动力剂。我们确定了一系列N-甲基苯胺衍生物作为新型非大环内酯 GPR38 激动剂。其中，12 -l-酒石酸盐（DS-3801b）被选为临床候选物进行进一步评估。

更新日期：2022-01-21

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