Design, Synthesis, and Evaluation of Naphthalene-Sulfonamide Antagonists of Human CCR8

Design, Synthesis, and Evaluation of Naphthalene-Sulfonamide Antagonists of Human CCR8

The design, synthesis, and structure−activity relationship development of naphthalene-derived human CCR8 antagonists is described. In vitro binding assay results of these investigations are reported, critical interactions of the antagonists with CCR8 are defined, and preliminary physicochemical and...

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Veröffentlicht in:Journal of medicinal chemistry 2007-02, Vol.50 (3), p.566-584
Hauptverfasser: Jenkins, Tracy J, Guan, Bing, Dai, Mingshi, Li, Gang, Lightburn, Thomas E, Huang, Shan, Freeze, B. Scott, Burdi, Douglas F, Jacutin-Porte, Swanee, Bennett, Robert, Chen, Weirong, Minor, Charles, Ghosh, Shomir, Blackburn, Christopher, Gigstad, Kenneth M, Jones, Matthew, Kolbeck, Roland, Yin, Wei, Smith, Sean, Cardillo, Daniel, Ocain, Timothy D, Harriman, Geraldine C
Format: Artikel
Sprache:eng
Schlagworte:
Administration, Oral
Animals
Biological and medical sciences
Biological Availability
Biological Transport
Calcium - metabolism
Cell Line
Cricetinae
Cricetulus
Drug Design
Humans
Medical sciences
Miscellaneous
Naphthalenes - chemical synthesis
Naphthalenes - pharmacokinetics
Naphthalenes - pharmacology
Pharmacology. Drug treatments
Rats
Receptors, CCR8
Receptors, Chemokine - antagonists & inhibitors
Solubility
Stereoisomerism
Structure-Activity Relationship
Sulfonamides - chemical synthesis
Sulfonamides - pharmacokinetics
Sulfonamides - pharmacology
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Beschreibung
Zusammenfassung:The design, synthesis, and structure−activity relationship development of naphthalene-derived human CCR8 antagonists is described. In vitro binding assay results of these investigations are reported, critical interactions of the antagonists with CCR8 are defined, and preliminary physicochemical and pharmacokinetic data for the naphthalene scaffold are presented.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm061118e