Literature DB >> 20444602

Anthranilic acid replacements in a niacin receptor agonist.

Darby Schmidt1, Abigail Smenton, Subharekha Raghavan, Hong Shen, Fa-Xiang Ding, Ester Carballo-Jane, Silvi Luell, 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. However, niacin must be taken in large doses and significant side effects are often observed, including facial flushing, loss of glucose tolerance, and liver toxicity. An anthranilic acid was identified as an agonist of the niacin receptor. In order to improve efficacy and provide structural diversity, replacements for the anthranilic acid were investigated and several compounds with improved properties were identified. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20444602     DOI: 10.1016/j.bmcl.2010.04.001

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


  2 in total

1.  One-pot synthesis of densely functionalized cyclic β-aminoesters containing four stereocenters, based on a Et3N-promoted pseudo five-component reaction.

Authors:  Juan Yao; Lanxiang Zhou; Chen Tan; Cunde Wang
Journal:  Mol Divers       Date:  2014-09-26       Impact factor: 2.943

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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