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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.

Authors+Show Affiliations

Medicinal Chemistry, Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, CA 92121, USA. pskinner@arenapharm.comNo 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 availableNo affiliation info availableNo affiliation info available

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/Fluorinated_pyrazole_acids_are_agonists_of_the_high_affinity_niacin_receptor_GPR109a_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0960-894X(07)00907-9 DB - PRIME DP - Unbound Medicine ER -