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Bioorg Med Chem Lett. 2013 Jan 1;23(1):194-7. doi: 10.1016/j.bmcl.2012.10.119. Epub 2012 Nov 5.

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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1
Pfizer Worldwide Research & Development, Groton Laboratories, Eastern Point Rd, Groton, CT 06340, United States. Kentaro.futatsugi@pfizer.com

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).

PMID:
23177788
DOI:
10.1016/j.bmcl.2012.10.119
[Indexed for MEDLINE]
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