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

  • Bioorg Med Chem Lett. 2012 Mar 15;22(6):2271-8. doi: 10.1016/j.bmcl.2012.01.078.
Patrick Hanrahan  1 ,  James Bell ,  Gillian Bottomley ,  Stuart Bradley ,  Phillip Clarke ,  Eleanor Curtis ,  Susan Davis ,  Graham Dawson ,  James Horswill ,  John Keily ,  Gary Moore ,  Chrystelle Rasamison ,  Jason Bloxham
Affiliations
PMID: 22342626 DOI: 10.1016/j.bmcl.2012.01.078
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.

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