1416137-41-1Relevant articles and documents
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
Futatsugi, Kentaro,Mascitti, Vincent,Guimar?es, Cristiano R.W.,Morishita, Nao,Cai, Cuiman,Deninno, Michael P.,Gao, Hua,Hamilton, Michael D.,Hank, Richard,Harris, Anthony R.,Kung, Daniel W.,Lavergne, Sophie Y.,Lefker, Bruce A.,Lopaze, Michael G.,McClure, Kim F.,Munchhof, Michael J.,Preville, Cathy,Robinson, Ralph P.,Wright, Stephen W.,Bonin, Paul D.,Cornelius, Peter,Chen, Yue,Kalgutkar, Amit S.
, p. 194 - 197 (2013/02/25)
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 GPR119 agonist 1. The design is centered on the conformational restriction of the core scaffold, while minimizing the change in spatial relationships of two key pharmacophoric elements (piperidine-carbamate and aryl sulfone).
