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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: diaz jl. 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
Acyl dipeptides as reversible caspase inhibitors. Part 2: further optimization.
Linton SD, Karanewsky DS, Ternansky RJ, Chen N, Guo X, Jahangiri KG, Kalish VJ, Meduna SP, Robinson ED, Ullman BR, Wu JC, Pham B, Kodandapani L, Smidt R, Diaz JL, Fritz LC, von Krosigk U, Roggo S, Schmitz A, Tomaselli KJ. Linton SD, et al. Among authors: diaz jl. Bioorg Med Chem Lett. 2002 Oct 21;12(20):2973-5. doi: 10.1016/s0960-894x(02)00630-3. Bioorg Med Chem Lett. 2002. PMID: 12270186
Structure-activity relationships within a series of caspase inhibitors: effect of leaving group modifications.
Ullman BR, Aja T, Deckwerth TL, Diaz JL, Herrmann J, Kalish VJ, Karanewsky DS, Meduna SP, Nalley K, Robinson ED, Roggo SP, Sayers RO, Schmitz A, Ternansky RJ, Tomaselli KJ, Wu JC. Ullman BR, et al. Among authors: diaz jl. Bioorg Med Chem Lett. 2003 Oct 20;13(20):3623-6. doi: 10.1016/s0960-894x(03)00755-8. Bioorg Med Chem Lett. 2003. PMID: 14505683
Oxamyl dipeptide caspase inhibitors developed for the treatment of stroke.
Linton SD, Aja T, Allegrini PR, Deckwerth TL, Diaz JL, Hengerer B, Herrmann J, Jahangiri KG, Kallen J, Karanewsky DS, Meduna SP, Nalley K, Robinson ED, Roggo S, Rovelli G, Sauter A, Sayers RO, Schmitz A, Smidt R, Ternansky RJ, Tomaselli KJ, Ullman BR, Wiessner C, Wu JC. Linton SD, et al. Among authors: diaz jl. Bioorg Med Chem Lett. 2004 May 17;14(10):2685-91. doi: 10.1016/j.bmcl.2003.12.106. Bioorg Med Chem Lett. 2004. PMID: 15109679
Structure-activity relationships within a series of caspase inhibitors. Part 2: Heterocyclic warheads.
Ullman BR, Aja T, Chen N, Diaz JL, Gu X, Herrmann J, Kalish VJ, Karanewsky DS, Kodandapani L, Krebs JJ, Linton SD, Meduna SP, Nalley K, Robinson ED, Roggo SP, Sayers RO, Schmitz A, Ternansky RJ, Tomaselli KJ, Wu JC. Ullman BR, et al. Among authors: diaz jl. Bioorg Med Chem Lett. 2005 Aug 1;15(15):3632-6. doi: 10.1016/j.bmcl.2005.05.036. Bioorg Med Chem Lett. 2005. PMID: 15964758
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: diaz jl. J Med Chem. 2008 Feb 14;51(3):400-6. doi: 10.1021/jm070623o. Epub 2008 Jan 12. J Med Chem. 2008. PMID: 18189346
188 results