Discovery and optimization of N-(3-(1,3-dioxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-4-yloxy)phenyl)benzenesulfonamides as novel GPR119 agonists |
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| Institution: | 1. Key Laboratory of Plant Resources Conservation and Sustainable Utilization, South China Botanical Garden, Chinese Academy of Sciences, Guangzhou 510650, China;2. Guangdong Provincial Key Laboratory of Applied Botany, South China Botanical Garden, Chinese Academy of Sciences, Guangzhou 510650, China;3. University of Chinese Academy of Sciences, Beijing 100049, China;4. School of Marine Sciences, Sun Yat-Sen University, Guangzhou 510006, China |
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| Abstract: | The discovery and optimization of novel N-(3-(1,3-dioxo-2,3-dihydro-1H-pyrrolo3,4-c]pyridin-4-yloxy)phenyl)benzenesulfonamide GPR119 agonists is described. Modification of the pyridylphthalimide motif of the molecule with R1 = –Me and R2 = –iPr substituents, incorporated with a 6-fluoro substitution on the central phenyl ring offered a potent and metabolically stable tool compound 22. |
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| Keywords: | GPR119 Agonist Type 2 diabetes |
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