Bioorganic and Medicinal Chemistry Letters p. 2100 - 2106 (2019)
Update date:2022-08-04
Topics:
Harada, Kazuhito
Mizukami, Jun
Watanabe, Takashi
Mori
Ubukata, Minoru
Suwa, Katsunori
Fukuda, Sumiaki
Negoro, Tamotsu
Sato, Motohide
Inaba, Takashi
We describe here a novel GPR119 agonist 24, which showed a potent and long-acting hypoglycemic effect in rats via oral dosing. For the discovery of 24, we chose compound 5, which possessed an oxadiazole linker, as a lead compound among our spirocyclic cyclohexane GPR119 agonist series, taking into account its lower plasma protein binding nature. 3,5-Difluoro and 4-methylsulfonylmethy groups on the left side phenyl group, and a gem-difluoro group on the right side of 24 are important for its agonist potency and metabolic stability, respectively.
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