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Pyrazole acids as niacin receptor agonists for the treatment of dyslipidemia.
Schmidt, Darby; Smenton, Abigail; Raghavan, Subharekha; Carballo-Jane, Ester; Lubell, Silvi; Ciecko, Tanya; Holt, Tom G; Wolff, Michael; Taggart, Andrew; Wilsie, Larissa; Krsmanovic, Mihajlo; Ren, Ning; Blom, Daniel; Cheng, Kang; McCann, Peggy E; Gerard Waters, M; Tata, James; Colletti, Steven.
Afiliação
  • Schmidt D; Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co, Inc, Rahway, NJ 07065-0900, USA. darbyrschmidt@verizon.net
Bioorg Med Chem Lett ; 19(16): 4768-72, 2009 Aug 15.
Article em En | MEDLINE | ID: mdl-19592242
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.
Assuntos

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Pirazóis / Agonistas Nicotínicos / Dislipidemias / Hipolipemiantes / Niacina Limite: Animals Idioma: En Ano de publicação: 2009 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Pirazóis / Agonistas Nicotínicos / Dislipidemias / Hipolipemiantes / Niacina Limite: Animals Idioma: En Ano de publicação: 2009 Tipo de documento: Article