From partial to full agonism: Identification of a novel 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole as a full agonist of the human GPR119 receptor
作者： Kentaro Futatsugi , Vincent Mascitti , Cristiano R.W. Guimarães , Nao Morishita , Cuiman Cai
DOI: 10.1016/J.BMCL.2012.10.119
关键词:
摘要: A novel GPR119 agonist based on the 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole scaffold was designed through lead optimization starting from pyrazole-based 1. The design is centered conformational restriction of core scaffold, while minimizing change in spatial relationships two key pharmacophoric elements (piperidine-carbamate and aryl sulfone).
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