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 |
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| Authors: | Kentaro Futatsugi Vincent Mascitti Cristiano R.W. Guimarães Nao Morishita Cuiman Cai Michael P. DeNinno Hua Gao Michael D. Hamilton Richard Hank Anthony R. Harris Daniel W. Kung Sophie Y. Lavergne Bruce A. Lefker Michael G. Lopaze Kim F. McClure Michael J. Munchhof Cathy Preville Ralph P. Robinson Amit S. Kalgutkar |
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| Affiliation: | Pfizer Worldwide Research & Development, Groton Laboratories, Eastern Point Rd, Groton, CT 06340, United States |
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| Abstract: | 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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