1.
Bioorg Med Chem Lett
; 19(16): 4768-72, 2009 Aug 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-19592242
RESUMEN
Niacin is an effective drug for raising HDL cholesterol and reducing coronary risks, but patients show low compliance with treatment due to severe facial flushing upon taking the drug. A series of bicyclic pyrazole carboxylic acids were synthesized and tested for their ability to activate the niacin receptor. One analog, 23, showed improved potency and lacked flushing at doses that effectively altered the lipid profile of rats.
Asunto(s)
Dislipidemias/tratamiento farmacológico , Hipolipemiantes/farmacología , Niacina/farmacología , Agonistas Nicotínicos/farmacología , Pirazoles/farmacología , Animales , HDL-Colesterol/metabolismo , Ácidos Grasos no Esterificados/metabolismo , Hipolipemiantes/síntesis química , Hipolipemiantes/química , Ratones , Niacina/química , Agonistas Nicotínicos/síntesis química , Agonistas Nicotínicos/química , Pirazoles/síntesis química , Pirazoles/química , Ratas , Receptores Acoplados a Proteínas G/agonistas , Receptores Acoplados a Proteínas G/metabolismo
2.
Bioorg Med Chem Lett
; 19(8): 2121-4, 2009 Apr 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-19307116
RESUMEN
5-Alkyl and aryl-pyrazole-tetrazoles have been identified as a new class of selective, small-molecule, agonists of the human G-protein-coupled receptor GPR109a, a high affinity receptor for the HDL-raising drug nicotinic acid.