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BIBTEX RIS

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

2012; Elsevier BV; Volume: 23; Issue: 1 Linguagem: Inglês

10.1016/j.bmcl.2012.10.119

ISSN

1464-3405

Autores

Kentaro Futatsugi, Vincent Mascitti, Cristiano R. W. Guimarães, Nao Morishita, Cuiman Cai, Michael P. DeNinno, Hua Gao, M. D. Hamilton, Richard F. Hank, Anthony R. Harris, Daniel W. Kung, Sophie Y. Lavergne, Bruce A. Lefker, Michael G. Lopaze, Kim F. McClure, Michael J. Munchhof, Cathy Préville, Ralph P. Robinson, Stephen W. Wright, Paul D. Bonin, Peter Cornelius, Yue Chen, Amit S. Kalgutkar,

Tópico(s)

Drug Transport and Resistance Mechanisms

Resumo

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).

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