Tags

Type your tag names separated by a space and hit enter

Fluorinated pyrazole acids are agonists of the high affinity niacin receptor GPR109a.
Bioorg Med Chem Lett. 2007 Oct 15; 17(20):5620-3.BM

Abstract

A series of 5-alkyl pyrazole-3-carboxylic acids were prepared and found to act as potent and selective agonists of the human GPCR, GPR109a, the high affinity nicotinic acid receptor. No activity was observed at the highly homologous low affinity niacin receptor, GPR109b. A further series of 4-fluoro-5-alkyl pyrazole-3-carboxylic acids were shown to display similar potency. One example from the series was shown to have improved properties in vivo compared to niacin.

Links

Publisher Full Text

Authors+Show Affiliations

Skinner PJ
Medicinal Chemistry, Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, CA 92121, USA. pskinner@arenapharm.com
Cherrier MC
No affiliation info available
Webb PJ
No affiliation info available
Shin YJ
No affiliation info available
Gharbaoui T
No affiliation info available
Lindstrom A
No affiliation info available
Hong V
No affiliation info available
Tamura SY
No affiliation info available
Dang HT
No affiliation info available
Pride CC
No affiliation info available
Chen R
No affiliation info available
Richman JG
No affiliation info available
Connolly DT
No affiliation info available
Semple G
No affiliation info available

MeSH

AcidsAnimalsFatty AcidsFluorineLigandsMaleMiceMolecular StructureNicotinic AgonistsPyrazolesRatsReceptors, G-Protein-CoupledReceptors, NicotinicStructure-Activity Relationship

Pub Type(s)

Journal Article

Language

eng

PubMed ID

17804224

Citation

Skinner, Philip J., et al. "Fluorinated Pyrazole Acids Are Agonists of the High Affinity Niacin Receptor GPR109a." Bioorganic & Medicinal Chemistry Letters, vol. 17, no. 20, 2007, pp. 5620-3.
Skinner PJ, Cherrier MC, Webb PJ, et al. Fluorinated pyrazole acids are agonists of the high affinity niacin receptor GPR109a. Bioorg Med Chem Lett. 2007;17(20):5620-3.
Skinner, P. J., Cherrier, M. C., Webb, P. J., Shin, Y. J., Gharbaoui, T., Lindstrom, A., Hong, V., Tamura, S. Y., Dang, H. T., Pride, C. C., Chen, R., Richman, J. G., Connolly, D. T., & Semple, G. (2007). Fluorinated pyrazole acids are agonists of the high affinity niacin receptor GPR109a. Bioorganic & Medicinal Chemistry Letters, 17(20), 5620-3.
Skinner PJ, et al. Fluorinated Pyrazole Acids Are Agonists of the High Affinity Niacin Receptor GPR109a. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5620-3. PubMed PMID: 17804224.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Fluorinated pyrazole acids are agonists of the high affinity niacin receptor GPR109a. AU - Skinner,Philip J, AU - Cherrier,Martin C, AU - Webb,Peter J, AU - Shin,Young-Jun, AU - Gharbaoui,Tawfik, AU - Lindstrom,Andrew, AU - Hong,Vu, AU - Tamura,Susan Y, AU - Dang,Huong T, AU - Pride,Cameron C, AU - Chen,Ruoping, AU - Richman,Jeremy G, AU - Connolly,Daniel T, AU - Semple,Graeme, Y1 - 2007/08/23/ PY - 2007/06/01/received PY - 2007/07/23/revised PY - 2007/07/24/accepted PY - 2007/9/7/pubmed PY - 2007/12/13/medline PY - 2007/9/7/entrez SP - 5620 EP - 3 JF - Bioorganic & medicinal chemistry letters JO - Bioorg Med Chem Lett VL - 17 IS - 20 N2 - A series of 5-alkyl pyrazole-3-carboxylic acids were prepared and found to act as potent and selective agonists of the human GPCR, GPR109a, the high affinity nicotinic acid receptor. No activity was observed at the highly homologous low affinity niacin receptor, GPR109b. A further series of 4-fluoro-5-alkyl pyrazole-3-carboxylic acids were shown to display similar potency. One example from the series was shown to have improved properties in vivo compared to niacin. SN - 0960-894X UR - https://www.unboundmedicine.com/medline/citation/17804224 L2 - https://linkinghub.elsevier.com/retrieve/pii/S0960-894X(07)00907-9 DB - PRIME DP - Unbound Medicine ER -
Grapherence [↓3]

Related Citations

    More

    Others Viewed