2. Academic Validation
  3. Analogues of acifran: agonists of the high and low affinity niacin receptors, GPR109a and GPR109b

Analogues of acifran: agonists of the high and low affinity niacin receptors, GPR109a and GPR109b

  • J Med Chem. 2007 Apr 5;50(7):1445-8. doi: 10.1021/jm070022x.
Jae-Kyu Jung 1,  Benjamin R Johnson,  Tracy Duong,  Marc Decaire,  Jane Uy,  Tawfik Gharbaoui,  P Douglas Boatman,  Carleton R Sage,  Ruoping Chen,  Jeremy G Richman,  Daniel T Connolly,  Graeme Semple
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, California 92121, USA.
PMID: 17358052 DOI: 10.1021/jm070022x
Abstract

Recently identified GPCRs, GPR109A and GPR109b, the high and low affinity receptors for niacin, may represent good targets for the development of HDL elevating drugs for the treatment of atherosclerosis. Acifran, an agonist of both receptors, has been tested in human subjects, yet until recently very few analogs had been reported. We describe a series of acifran analogs prepared using newly developed synthetic pathways and evaluated as agonists for GPR109A and GPR109b, resulting in identification of compounds with improved activity at these receptors.

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