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Bioorg Med Chem Lett. 2007 Sep 1;17(17):4914-9. Epub 2007 Jun 10.

Agonist lead identification for the high affinity niacin receptor GPR109a.

Author information

1
Department of Medicinal Chemistry, Arena Pharmaceuticals, San Diego, CA 92121, USA.

Abstract

A strategy for lead identification of new agonists of GPR109a, starting from known compounds shown to activate the receptor, is described. Early compound triage led to the formulation of a binding hypothesis and eventually to our focus on a series of pyrazole acid derivatives. Further elaboration of these compounds provided a series of 5,5-fused pyrazoles to be used as lead compounds for further optimization.

PMID:
17588745
DOI:
10.1016/j.bmcl.2007.06.028
[Indexed for MEDLINE]

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