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Discovery of novel pyrrole derivatives as potent agonists for the niacin receptor GPR109A
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2020-03-10 , DOI: 10.1016/j.bmcl.2020.127105 Yuriko Miyazawa , Takahiro Yamaguchi , Mitsuhiro Yamaguchi , Keiko Tago , Akihiro Tamura , Daisuke Sugiyama , Takahide Aburatani , Tomohiro Nishizawa , Nobuya Kurikawa , Keita Kono
中文翻译：
发现新的吡咯衍生物作为烟酸受体GPR109A的有效激动剂
更新日期：2020-03-12
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2020-03-10 , DOI: 10.1016/j.bmcl.2020.127105 Yuriko Miyazawa , Takahiro Yamaguchi , Mitsuhiro Yamaguchi , Keiko Tago , Akihiro Tamura , Daisuke Sugiyama , Takahide Aburatani , Tomohiro Nishizawa , Nobuya Kurikawa , Keita Kono
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Novel pyrrole derivatives were discovered as potent agonists of the niacin receptor, GPR109A. During the derivatization, compound 16 was found to be effective both in vitro and in vivo. The compound 16 exhibited a significant reduction of the non-esterified fatty acid in human GPR109A transgenic rats, and the duration of its in vivo efficacy was much longer than niacin.
中文翻译：
发现新的吡咯衍生物作为烟酸受体GPR109A的有效激动剂
发现新的吡咯衍生物作为烟酸受体GPR109A的有效激动剂。在衍生过程中，发现化合物16在体外和体内均有效。化合物16在人GPR109A转基因大鼠中显示出非酯化脂肪酸的显着减少，并且其体内功效的持续时间比烟酸长得多。
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