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Bioorg Med Chem Lett. 2009 Aug 15;19(16):4768-72. doi: 10.1016/j.bmcl.2009.06.054. Epub 2009 Jun 17.

Pyrazole acids as niacin receptor agonists for the treatment of dyslipidemia.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co, Inc, Rahway, NJ 07065-0900, USA. darbyrschmidt@verizon.net

Abstract

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.

PMID:
19592242
DOI:
10.1016/j.bmcl.2009.06.054
[Indexed for MEDLINE]

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