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Page 1
Identification of novel, water-soluble, 2-amino-N-pyrimidin-4-yl acetamides as A2A receptor antagonists with in vivo efficacy.
Slee DH, Zhang X, Moorjani M, Lin E, Lanier MC, Chen Y, Rueter JK, Lechner SM, Markison S, Malany S, Joswig T, Santos M, Gross RS, Williams JP, Castro-Palomino JC, Crespo MI, Prat M, Gual S, Díaz JL, Wen J, O'Brien Z, Saunders J. Slee DH, et al. Among authors: lin e. J Med Chem. 2008 Feb 14;51(3):400-6. doi: 10.1021/jm070623o. Epub 2008 Jan 12. J Med Chem. 2008. PMID: 18189346
2,6-Diaryl-4-phenacylaminopyrimidines as potent and selective adenosine A(2A) antagonists with reduced hERG liability.
Moorjani M, Zhang X, Chen Y, Lin E, Rueter JK, Gross RS, Lanier MC, Tellew JE, Williams JP, Lechner SM, Malany S, Santos M, Ekhlassi P, Castro-Palomino JC, Crespo MI, Prat M, Gual S, Díaz JL, Saunders J, Slee DH. Moorjani M, et al. Among authors: lin e. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1269-73. doi: 10.1016/j.bmcl.2008.01.036. Epub 2008 Jan 13. Bioorg Med Chem Lett. 2008. PMID: 18249540
2-Amino-N-pyrimidin-4-ylacetamides as A2A receptor antagonists: 1. Structure-activity relationships and optimization of heterocyclic substituents.
Slee DH, Chen Y, Zhang X, Moorjani M, Lanier MC, Lin E, Rueter JK, Williams JP, Lechner SM, Markison S, Malany S, Santos M, Gross RS, Jalali K, Sai Y, Zuo Z, Yang C, Castro-Palomino JC, Crespo MI, Prat M, Gual S, Díaz JL, Saunders J. Slee DH, et al. Among authors: lin e. J Med Chem. 2008 Mar 27;51(6):1719-29. doi: 10.1021/jm701185v. Epub 2008 Feb 29. J Med Chem. 2008. PMID: 18307292
2-Amino-N-pyrimidin-4-ylacetamides as A2A receptor antagonists: 2. Reduction of hERG activity, observed species selectivity, and structure-activity relationships.
Slee DH, Moorjani M, Zhang X, Lin E, Lanier MC, Chen Y, Rueter JK, Lechner SM, Markison S, Malany S, Joswig T, Santos M, Gross RS, Williams JP, Castro-Palomino JC, Crespo MI, Prat M, Gual S, Díaz JL, Jalali K, Sai Y, Zuo Z, Yang C, Wen J, O'Brien Z, Petroski R, Saunders J. Slee DH, et al. Among authors: lin e. J Med Chem. 2008 Mar 27;51(6):1730-9. doi: 10.1021/jm701187w. Epub 2008 Feb 29. J Med Chem. 2008. PMID: 18307293
Synthesis of N-pyrimidinyl-2-phenoxyacetamides as adenosine A2A receptor antagonists.
Zhang X, Rueter JK, Chen Y, Moorjani M, Lanier MC, Lin E, Gross RS, Tellew JE, Williams JP, Lechner SM, Markison S, Joswig T, Malany S, Santos M, Castro-Palomino JC, Crespo MI, Prat M, Gual S, Díaz JL, Saunders J, Slee DH. Zhang X, et al. Among authors: lin e. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1778-83. doi: 10.1016/j.bmcl.2008.02.032. Epub 2008 Feb 16. Bioorg Med Chem Lett. 2008. PMID: 18329269
2,6-Diaryl-4-acylaminopyrimidines as potent and selective adenosine A(2A) antagonists with improved solubility and metabolic stability.
Moorjani M, Luo Z, Lin E, Vong BG, Chen Y, Zhang X, Rueter JK, Gross RS, Lanier MC, Tellew JE, Williams JP, Lechner SM, Malany S, Santos M, Crespo MI, Díaz JL, Saunders J, Slee DH. Moorjani M, et al. Among authors: lin e. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5402-5. doi: 10.1016/j.bmcl.2008.09.048. Epub 2008 Sep 14. Bioorg Med Chem Lett. 2008. PMID: 18835161
Lead optimization of 4-acetylamino-2-(3,5-dimethylpyrazol-1-yl)-6-pyridylpyrimidines as A2A adenosine receptor antagonists for the treatment of Parkinson's disease.
Zhang X, Tellew JE, Luo Z, Moorjani M, Lin E, Lanier MC, Chen Y, Williams JP, Saunders J, Lechner SM, Markison S, Joswig T, Petroski R, Piercey J, Kargo W, Malany S, Santos M, Gross RS, Wen J, Jalali K, O'Brien Z, Stotz CE, Crespo MI, Díaz JL, Slee DH. Zhang X, et al. Among authors: lin e. J Med Chem. 2008 Nov 27;51(22):7099-110. doi: 10.1021/jm800851u. J Med Chem. 2008. PMID: 18947224
N-[6-amino-2-(heteroaryl)pyrimidin-4-yl]acetamides as A2A receptor antagonists with improved drug like properties and in vivo efficacy.
Lanier MC, Moorjani M, Luo Z, Chen Y, Lin E, Tellew JE, Zhang X, Williams JP, Gross RS, Lechner SM, Markison S, Joswig T, Kargo W, Piercey J, Santos M, Malany S, Zhao M, Petroski R, Crespo MI, Díaz JL, Saunders J, Wen J, O'Brien Z, Jalali K, Madan A, Slee DH. Lanier MC, et al. Among authors: lin e. J Med Chem. 2009 Feb 12;52(3):709-17. doi: 10.1021/jm800908d. J Med Chem. 2009. PMID: 19140664
Discovery of NBI-77860/GSK561679, a potent corticotropin-releasing factor (CRF1) receptor antagonist with improved pharmacokinetic properties.
Tellew JE, Lanier M, Moorjani M, Lin E, Luo Z, Slee DH, Zhang X, Hoare SR, Grigoriadis DE, St Denis Y, Di Fabio R, Di Modugno E, Saunders J, Williams JP. Tellew JE, et al. Among authors: lin e. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7259-64. doi: 10.1016/j.bmcl.2010.10.095. Epub 2010 Oct 25. Bioorg Med Chem Lett. 2010. PMID: 21074436
2,787 results