Scaffold-hopping with zwitterionic CCR3 antagonists: Identification and optimisation of a series with good potency and pharmacokinetics leading to the discovery of AZ12436092
2012
Bahl, Ash | Barton, Patrick | Bowers, Keith | Caffrey, Moya V. | Denton, Rebecca | Gilmour, Peter | Hawley, Shaun | Linannen, Tero | Luckhurst, Christopher A. | Mochel, Tobias | Perry, Matthew W.D. | Riley, Robert J. | Roe, Emma | Springthorpe, Brian | Stein, Linda | Webborn, Peter
The discovery and optimisation of a series of zwitterionic CCR3 antagonists is described. Optimisation of the structure led to AZ12436092, a compound with excellent selectivity over activity at hERG and outstanding pharmacokinetics in preclinical species.
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