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Page 1
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. 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
Discovery of N-propylurea 3-benzylpiperidines as selective CC chemokine receptor-3 (CCR3) antagonists.
Varnes JG, Gardner DS, Santella JB 3rd, Duncia JV, Estrella M, Watson PS, Clark CM, Ko SS, Welch P, Covington M, Stowell N, Wadman E, Davies P, Solomon K, Newton RC, Trainor GL, Decicco CP, Wacker DA. Varnes JG, et al. Among authors: wacker da. Bioorg Med Chem Lett. 2004 Apr 5;14(7):1645-9. doi: 10.1016/j.bmcl.2004.01.059. Bioorg Med Chem Lett. 2004. PMID: 15026042
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: wacker da. 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
Discovery of (R)-9-ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2,1-a]isoindol- 6(2H)-one, a selective, orally active agonist of the 5-HT(2C) receptor.
Wacker DA, Varnes JG, Malmstrom SE, Cao X, Hung CP, Ung T, Wu G, Zhang G, Zuvich E, Thomas MA, Keim WJ, Cullen MJ, Rohrbach KW, Qu Q, Narayanan R, Rossi K, Janovitz E, Lehman-McKeeman L, Malley MF, Devenny J, Pelleymounter MA, Miller KJ, Robl JA. Wacker DA, et al. J Med Chem. 2007 Mar 22;50(6):1365-79. doi: 10.1021/jm0612968. Epub 2007 Feb 23. J Med Chem. 2007. PMID: 17315987
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: wacker da. J Med Chem. 2005 Mar 24;48(6):2194-211. doi: 10.1021/jm049530m. J Med Chem. 2005. PMID: 15771462
Position 5.46 of the serotonin 5-HT2A receptor contributes to a species-dependent variation for the 5-HT2C agonist (R)-9-ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2,1-a]isoindol-6(2H)-one: impact on selectivity and toxicological evaluation.
Miller KJ, Wu GY, Varnes JG, Levesque P, Li J, Li D, Robl JA, Rossi KA, Wacker DA. Miller KJ, et al. Among authors: wacker da. Mol Pharmacol. 2009 Dec;76(6):1211-9. doi: 10.1124/mol.109.059204. Epub 2009 Sep 18. Mol Pharmacol. 2009. PMID: 19767451
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: wacker da. 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
33 results