Evaluation of basic,heterocyclic ring systems as templates for use as potassium competitive acid blockers (pCABs) |
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| Authors: | Terry Panchal Nick Bailey Mark Bamford Emmanuel Demont Richard Elliott Irene Farre-Gutierrez Neil Garton Thomas Hayhow Gail Hutley Antoinette Naylor |
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| Affiliation: | Neurology and Gastrointestinal Centre of Excellence for Drug Discovery, GlaxoSmithKline R&D, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom |
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| 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. |
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