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Analogues of acifran: agonists of the high and low affinity niacin receptors, GPR109a and GPR109b.
J Med Chem. 2007 Apr 05; 50(7):1445-8.JM

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.

Authors+Show Affiliations

Department of Medicinal Chemistry, Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, California 92121, USA.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

17358052

Citation

Jung, Jae-Kyu, et al. "Analogues of Acifran: Agonists of the High and Low Affinity Niacin Receptors, GPR109a and GPR109b." Journal of Medicinal Chemistry, vol. 50, no. 7, 2007, pp. 1445-8.
Jung JK, Johnson BR, Duong T, et al. Analogues of acifran: agonists of the high and low affinity niacin receptors, GPR109a and GPR109b. J Med Chem. 2007;50(7):1445-8.
Jung, J. K., Johnson, B. R., Duong, T., Decaire, M., Uy, J., Gharbaoui, T., Boatman, P. D., Sage, C. R., Chen, R., Richman, J. G., Connolly, D. T., & Semple, G. (2007). Analogues of acifran: agonists of the high and low affinity niacin receptors, GPR109a and GPR109b. Journal of Medicinal Chemistry, 50(7), 1445-8.
Jung JK, et al. 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. PubMed PMID: 17358052.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Analogues of acifran: agonists of the high and low affinity niacin receptors, GPR109a and GPR109b. AU - Jung,Jae-Kyu, AU - Johnson,Benjamin R, AU - Duong,Tracy, AU - Decaire,Marc, AU - Uy,Jane, AU - Gharbaoui,Tawfik, AU - Boatman,P Douglas, AU - Sage,Carleton R, AU - Chen,Ruoping, AU - Richman,Jeremy G, AU - Connolly,Daniel T, AU - Semple,Graeme, Y1 - 2007/03/15/ PY - 2007/3/16/pubmed PY - 2007/5/15/medline PY - 2007/3/16/entrez SP - 1445 EP - 8 JF - Journal of medicinal chemistry JO - J Med Chem VL - 50 IS - 7 N2 - 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. SN - 0022-2623 UR - https://www.unboundmedicine.com/medline/citation/17358052/Analogues_of_acifran:_agonists_of_the_high_and_low_affinity_niacin_receptors_GPR109a_and_GPR109b_ L2 - https://doi.org/10.1021/jm070022x DB - PRIME DP - Unbound Medicine ER -