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CCR3 antagonists: a potential new therapy for the treatment of asthma. Discovery and structure-activity relationships |
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| Authors: | Wacker Dean A Santella Joseph B Gardner Daniel S Varnes Jeffrey G Estrella Melissa DeLucca George V Ko Soo S Tanabe Keiichi Watson Paul S Welch Patricia K Covington Maryanne Stowell Nicole C Wadman Eric A Davies Paul Solomon Kimberly A Newton Robert C Trainor George L Friedman Steven M Decicco Carl P Duncia John V |
| Institution: | Bristol-Myers Squibb Company, Experimental Station, PO Box 80336, Wilmington, DE 19880-0336, USA. dean.wacker@bms.com |
| Abstract: | CCR3 antagonist leads with IC(50) values in the microM range were converted into low nM binding compounds that displayed in vitro inhibition of human eosinophil chemotaxis induced by human eotaxin. In particular, 4-benzylpiperidin-1-yl-n-propylureas and erythro-3-(4-benzyl-2-(alpha-hydroxyalkyl)piperidin-1-yl)-n-propylureas (obtained via Beak reaction of N-BOC-4-benzylpiperidine) exhibited single digit nanomolar IC(50) values for CCR3. |
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