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PubMed 22342626


Referenced in: none

Automatically associated channels: Kv11.1



Title: Substituted azaquinazolinones as modulators of GHSr-1a for the treatment of type II diabetes and obesity.

Authors: Patrick Hanrahan, James Bell, Gillian Bottomley, Stuart Bradley, Phillip Clarke, Eleanor Curtis, Susan Davis, Graham Dawson, James Horswill, John Keily, Gary Moore, Chrystelle Rasamison, Jason Bloxham

Journal, date & volume: Bioorg. Med. Chem. Lett., 2012 Mar 15 , 22, 2271-8

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/22342626


Abstract
Substituted azaquinazolinones were identified as antagonists of the GHSr-1A receptor for the treatment of type II diabetes and obesity. Optimisation for potency and LogD lead to the identification of orally bioavailable, potent antagonists with improved selectivity over hERG.