Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2021-02-13 , DOI: 10.1016/j.bmc.2021.116071 Suresh Pola 1 , Shailesh R Shah 2 , Harikishore Pingali 3 , Pandurang Zaware 3 , Baban Thube 3 , Pankaj Makadia 3 , Hoshang Patel 3 , Debdutta Bandyopadhyay 3 , Akshyaya Rath 3 , Suresh Giri 3 , Jitendra H Patel 3 , R K Ranvir 3 , S R Sundar 3 , Harilal Patel 3 , Jeevan Kumar 3 , Mukul R Jain 3
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The ever-growing prevalence of Type-2 diabetes in the world has an urgent need for multiple orally effective agents that can regulate glucose homeostasis. G-Protein coupled receptor 119 (GPR 119) agonists have demonstrated the glucose-dependent insulin secretion and showed beneficial effects on glycemic control in humans and/or relevant animal models. Herein, we describe our efforts towards identification of a potent and oral GPR 119 agonist 13c (ZY-G19), which showed in vitro potency in the cell-based assay and in vivo efficacy without exerting any significant signs of toxicity in relevant animal models.
中文翻译：
发现用于治疗 2 型糖尿病的有效 G 蛋白偶联受体 119 激动剂
世界上 2 型糖尿病的患病率不断增加，迫切需要多种口服有效的药物来调节葡萄糖稳态。G-蛋白偶联受体 119 (GPR 119) 激动剂已证明葡萄糖依赖性胰岛素分泌，并在人类和/或相关动物模型中显示出对血糖控制的有益作用。在此，我们描述了我们为鉴定有效的口服 GPR 119 激动剂13c (ZY-G19)所做的努力，其在基于细胞的测定中显示出体外效力和体内功效，而在相关动物模型中没有表现出任何显着的毒性迹象。
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