GPR109a agonists. Part 2: pyrazole-acids as agonists of the human orphan G-protein coupled receptor GPR109a.

Imbriglio, Jason E; Chang, Sookhee; Liang, Rui; Raghavan, Subharekha; Schmidt, Darby; Smenton, Abby; Tria, Scott; Schrader, Thomas O; Jung, Jae-Kyu; Esser, Craig; Holt, Tom G; Wolff, Michael S; Taggart, Andrew K P; Cheng, Kang; Carballo-Jane, Ester; Waters, M Gerard; Tata, James R; Colletti, Steven L

Imbriglio, Jason E; Chang, Sookhee; Liang, Rui; Raghavan, Subharekha; Schmidt, Darby; Smenton, Abby; Tria, Scott; Schrader, Thomas O; Jung, Jae-Kyu; Esser, Craig; Holt, Tom G; Wolff, Michael S; Taggart, Andrew K P; Cheng, Kang; Carballo-Jane, Ester; Waters, M Gerard; Tata, James R; Colletti, Steven L.

Afiliación

Imbriglio JE; Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., Inc., Rahway, NJ 07065-0900, USA. jason_imbriglio@merck.com

Bioorg Med Chem Lett ; 20(15): 4472-4, 2010 Aug 01.

Article en En | MEDLINE | ID: mdl-20615702

ABSTRACT

ABSTRACT

5-Alkyl and aryl-pyrazole-acids have been identified as a new class of selective, small-molecule, agonists of the human orphan G-protein-coupled receptor GPR109a, a high affinity receptor for the HDL-raising drug nicotinic acid.

Asunto(s)

Pirazoles/química; Receptores Acoplados a Proteínas G/agonistas; Animales; Ácidos Grasos/metabolismo; Humanos; Ratones; Niacina/química; Pirazoles/síntesis química; Pirazoles/farmacocinética; Receptores Acoplados a Proteínas G/metabolismo; Receptores Nicotínicos/metabolismo

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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Pirazoles / Receptores Acoplados a Proteínas G Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2010 Tipo del documento: Article País de afiliación: Estados Unidos

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