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Racemic and chiral lactams as potent, selective and functionally active CCR4 antagonists
Authors:Newhouse Bradley  Allen Shelley  Fauber Benjamin  Anderson Aaron S  Eary C Todd  Hansen Joshua D  Schiro Justin  Gaudino John J  Laird Ellen  Chantry David  Eberhardt Christine  Burgess Laurence E
Affiliation:Array BioPharma, 3200 Walnut Street, Boulder, CO 80301, USA.
Abstract:A series of racemic and chiral, nonracemic lactams that display high binding affinities, functional chemotaxis antagonism, and selectivity toward CCR4 are described. Compound 41, which provides reasonably high blood levels in mice when dosed intraperitoneally, was identified as a useful pharmacological tool to explore the role of CCR4 antagonism in animal models of allergic disease.
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