1. Design, Synthesis, and Evaluation of Naphthalene-Sulfonamide Antagonists of Human CCR8
- Author
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Mingshi Dai, Swanee Jacutin-Porte, Wei Yin, Charles A. Minor, Shan Huang, Tracy J. Jenkins, Weirong Chen, Gang Li, Thomas E. Lightburn, Daniel Cardillo, Matthew Jones, Shomir Ghosh, Douglas F. Burdi, Christopher Blackburn, Robert Bennett, Roland Kolbeck, Sean Smith, B. Scott Freeze, Timothy D. Ocain, Geraldine C Harriman, Kenneth M. Gigstad, and Bing Guan
- Subjects
medicine.drug_class ,Stereochemistry ,Administration, Oral ,Biological Availability ,Stereoisomerism ,Carboxamide ,Naphthalenes ,Chemical synthesis ,Receptors, CCR8 ,Cell Line ,Structure-Activity Relationship ,chemistry.chemical_compound ,Cricetulus ,Cricetinae ,Drug Discovery ,medicine ,Animals ,Humans ,Structure–activity relationship ,Naphthalene ,chemistry.chemical_classification ,Sulfonamides ,Bicyclic molecule ,Biological Transport ,In vitro ,Rats ,Sulfonamide ,Solubility ,chemistry ,Drug Design ,Molecular Medicine ,Calcium ,Receptors, Chemokine - Abstract
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.
- Published
- 2007
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