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Page 1
N-Arylalkylpiperidine urea derivatives as CC chemokine receptor-3 (CCR3) antagonists.
Batt DG, Houghton GC, Roderick J, Santella JB 3rd, Wacker DA, Welch PK, Orlovsky YI, Wadman EA, Trzaskos JM, Davies P, Decicco CP, Carter PH. Batt DG, et al. Among authors: wadman ea. Bioorg Med Chem Lett. 2005 Feb 1;15(3):787-91. doi: 10.1016/j.bmcl.2004.11.006. Bioorg Med Chem Lett. 2005. PMID: 15664858
CC chemokine receptor-3 (CCR3) antagonists: improving the selectivity of DPC168 by reducing central ring lipophilicity.
Pruitt JR, Batt DG, Wacker DA, Bostrom LL, Booker SK, McLaughlin E, Houghton GC, Varnes JG, Christ DD, Covington M, Das AM, Davies P, Graden D, Kariv I, Orlovsky Y, Stowell NC, Vaddi KG, Wadman EA, Welch PK, Yeleswaram S, Solomon KA, Newton RC, Decicco CP, Carter PH, Ko SS. Pruitt JR, et al. Among authors: wadman ea. Bioorg Med Chem Lett. 2007 Jun 1;17(11):2992-7. doi: 10.1016/j.bmcl.2007.03.065. Epub 2007 Mar 24. Bioorg Med Chem Lett. 2007. PMID: 17418570
From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part II: Acyclic replacements for the (3S)-3-benzylpiperidine in a series of potent CCR3 antagonists.
Gardner DS, Santella JB 3rd, Tebben AJ, Batt DG, Ko SS, Traeger SC, Welch PK, Wadman EA, Davies P, Carter PH, Duncia JV. Gardner DS, et al. Among authors: wadman ea. Bioorg Med Chem Lett. 2008 Jan 15;18(2):586-95. doi: 10.1016/j.bmcl.2007.11.087. Epub 2007 Nov 28. Bioorg Med Chem Lett. 2008. PMID: 18160284
Discovery of CC chemokine receptor-3 (CCR3) antagonists with picomolar potency.
De Lucca GV, Kim UT, Vargo BJ, Duncia JV, Santella JB 3rd, Gardner DS, Zheng C, Liauw A, Wang Z, Emmett G, Wacker DA, Welch PK, Covington M, Stowell NC, Wadman EA, Das AM, Davies P, Yeleswaram S, Graden DM, Solomon KA, Newton RC, Trainor GL, Decicco CP, Ko SS. De Lucca GV, et al. Among authors: wadman ea. J Med Chem. 2005 Mar 24;48(6):2194-211. doi: 10.1021/jm049530m. J Med Chem. 2005. PMID: 15771462
CCR3 antagonists: a potential new therapy for the treatment of asthma. Discovery and structure-activity relationships.
Wacker DA, Santella JB 3rd, Gardner DS, Varnes JG, Estrella M, DeLucca GV, Ko SS, Tanabe K, Watson PS, Welch PK, Covington M, Stowell NC, Wadman EA, Davies P, Solomon KA, Newton RC, Trainor GL, Friedman SM, Decicco CP, Duncia JV. Wacker DA, et al. Among authors: wadman ea. Bioorg Med Chem Lett. 2002 Jul 8;12(13):1785-9. doi: 10.1016/s0960-894x(02)00206-8. Bioorg Med Chem Lett. 2002. PMID: 12067561
2,4-Disubstituted piperidines as selective CC chemokine receptor 3 (CCR3) antagonists: synthesis and selectivity.
Watson PS, Jiang B, Harrison K, Asakawa N, Welch PK, Covington M, Stowell NC, Wadman EA, Davies P, Solomon KA, Newton RC, Trainor GL, Friedman SM, Decicco CP, Ko SS. Watson PS, et al. Among authors: wadman ea. Bioorg Med Chem Lett. 2006 Nov 1;16(21):5695-9. doi: 10.1016/j.bmcl.2006.08.012. Epub 2006 Aug 23. Bioorg Med Chem Lett. 2006. PMID: 16931001
From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part I: the discovery of CCR3 antagonist development candidate BMS-639623 with picomolar inhibition potency against eosinophil chemotaxis.
Santella JB 3rd, Gardner DS, Yao W, Shi C, Reddy P, Tebben AJ, DeLucca GV, Wacker DA, Watson PS, Welch PK, Wadman EA, Davies P, Solomon KA, Graden DM, Yeleswaram S, Mandlekar S, Kariv I, Decicco CP, Ko SS, Carter PH, Duncia JV. Santella JB 3rd, et al. Among authors: wadman ea. Bioorg Med Chem Lett. 2008 Jan 15;18(2):576-85. doi: 10.1016/j.bmcl.2007.11.067. Epub 2007 Nov 22. Bioorg Med Chem Lett. 2008. PMID: 18096386
Selective inhibition of eosinophil influx into the lung by small molecule CC chemokine receptor 3 antagonists in mouse models of allergic inflammation.
Das AM, Vaddi KG, Solomon KA, Krauthauser C, Jiang X, McIntyre KW, Yang XX, Wadman E, Welch P, Covington M, Graden D, Yeleswaram K, Trzaskos JM, Newton RC, Mandlekar S, Ko SS, Carter PH, Davies P. Das AM, et al. J Pharmacol Exp Ther. 2006 Jul;318(1):411-7. doi: 10.1124/jpet.105.099812. Epub 2006 Apr 13. J Pharmacol Exp Ther. 2006. PMID: 16614169