2. Academic Validation
  3. Substituted azaquinazolinones as modulators of GHSr-1a for the treatment of type II diabetes and obesity

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

Affiliation

  • 1 Medicinal Chemistry, Prosidion Ltd, Oxford, United Kingdom. hanrahanpatrick@yahoo.co.uk
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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