The discovery of CCR3/H 1 dual antagonists with reduced hERG risk

A Bahl, P Barton, K Bowers, S Brough, R Evans…

文献索引：Barton, Patrick; Brough, Steven; Evans, Richard; Luckhurst, Christopher A.; Mochel, Tobias; Perry, Matthew W. D.; Rigby, Aaron; Sanganee, Hitesh; Sisson, Adam; Springthorpe, Brian; Bahl, Ash; Bowers, Keith; Riley, Robert J. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 21 p. 6688 - 6693,6

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被引用次数: 5

摘要

A series of dual CCR3/H1 antagonists based on a bispiperidine scaffold were discovered. Introduction of an acidic group overcame hERG liability. Bioavailability was optimised by modulation of physico-chemical properties and physical form to deliver a compound suitable for clinical evaluation.