Discovery of novel pyrrole derivatives as potent agonists for the niacin receptor GPR109A

Yuriko Miyazawa,Takahiro Yamaguchi,Mitsuhiro Yamaguchi,Keiko Tago,Akihiro Tamura,Daisuke Sugiyama,Takahide Aburatani,Tomohiro Nishizawa,Nobuya Kurikawa,Keita Kono

doi:10.1016/j.bmcl.2020.127105

Discovery of novel pyrrole derivatives as potent agonists for the niacin receptor GPR109A

Yuriko Miyazawa, Takahiro Yamaguchi + Show 8 more

Open Access

https://doi.org/10.1016/j.bmcl.2020.127105

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Journal: Bioorganic & Medicinal Chemistry Letters	Publication Date: Mar 10, 2020
Citations: 2	License type: cc-by

Affiliation: Daiichi-Sankyo (Japan)

#Pyrrole Derivatives #Niacin Receptor + Show 8 more

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Abstract

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.

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