Literature DB >> 19592242

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

Darby Schmidt1, Abigail Smenton, Subharekha Raghavan, Ester Carballo-Jane, Silvi Lubell, Tanya Ciecko, Tom G Holt, Michael Wolff, Andrew Taggart, Larissa Wilsie, Mihajlo Krsmanovic, Ning Ren, Daniel Blom, Kang Cheng, Peggy E McCann, M Gerard Waters, James Tata, Steven Colletti.   

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.

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Year:  2009        PMID: 19592242     DOI: 10.1016/j.bmcl.2009.06.054

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  A new palladium precatalyst allows for the fast Suzuki-Miyaura coupling reactions of unstable polyfluorophenyl and 2-heteroaryl boronic acids.

Authors:  Tom Kinzel; Yong Zhang; Stephen L Buchwald
Journal:  J Am Chem Soc       Date:  2010-10-13       Impact factor: 15.419

Review 2.  G protein-coupled receptors for energy metabolites as new therapeutic targets.

Authors:  Clara C Blad; Cong Tang; Stefan Offermanns
Journal:  Nat Rev Drug Discov       Date:  2012-07-13       Impact factor: 84.694

  2 in total

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