| Literature DB >> 19846298 |
Terry Panchal1, Nick Bailey, Mark Bamford, Emmanuel Demont, Richard Elliott, Irene Farre-Gutierrez, Neil Garton, Thomas Hayhow, Gail Hutley, Antoinette Naylor.
Abstract
A variety of basic, heterocyclic templates has been reported as potassium-competitive, acid pump antagonists. Herein, we report a comparison of potencies of these templates and others to establish which offers the best start point for further systematic optimisation. Modifications were carried out to improve the developability profile of the more potent 1H-pyrrolo[2,3-c]pyridine template, affording molecules with improved overall in vitro characteristics versus the reported clinical candidate AR-H047108, and comparable to the clinically efficacious AZD-0865.Entities:
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Year: 2009 PMID： 19846298 DOI： 10.1016/j.bmcl.2009.07.002
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823