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Racemic and chiral lactams as potent, selective and functionally active CCR4 antagonists.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2004 Nov 15; Vol. 14 (22), pp. 5537-42. - Publication Year :
- 2004
-
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.
- Subjects :
- Animals
Binding Sites
Binding, Competitive drug effects
Disease Models, Animal
Drug Evaluation, Preclinical
Hypersensitivity drug therapy
Lactams chemical synthesis
Mice
Molecular Structure
Receptors, CCR4
Stereoisomerism
Structure-Activity Relationship
Lactams chemistry
Lactams pharmacokinetics
Receptors, Chemokine antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 14
- Issue :
- 22
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 15482919
- Full Text :
- https://doi.org/10.1016/j.bmcl.2004.09.001