The insulin secretory action of novel polycyclic guanidines: Discovery through open innovation phenotypic screening, and exploration of structure–activity …

MB Shaghafi, DG Barrett, FS Willard…

文献索引：Shaghafi, Michael B.; Barrett, David G.; Willard, Francis S.; Overman, Larry E. Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 4 p. 1031 - 1036

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被引用次数: 6

摘要

Abstract We report the discovery of the glucose-dependent insulin secretogogue activity of a novel class of polycyclic guanidines through phenotypic screening as part of the Lilly Open Innovation Drug Discovery platform. Three compounds from the University of California, Irvine, 1–3, having the 3-arylhexahydropyrrolo [1, 2-c] pyrimidin-1-amine scaffold acted as insulin secretagogues under high, but not low, glucose conditions. Exploration of the ...