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Page 1
Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: structure-activity relationship of the aryl region.
Probst GD, Bowers S, Sealy JM, Stupi B, Dressen D, Jagodzinska BM, Aquino J, Gailunas A, Truong AP, Tso L, Xu YZ, Hom RK, John V, Tung JS, Pleiss MA, Tucker JA, Konradi AW, Sham HL, Jagodzinski J, Toth G, Brecht E, Yao N, Pan H, Lin M, Artis DR, Ruslim L, Bova MP, Sinha S, Yednock TA, Gauby S, Zmolek W, Quinn KP, Sauer JM. Probst GD, et al. Among authors: tucker ja. Bioorg Med Chem Lett. 2010 Oct 15;20(20):6034-9. doi: 10.1016/j.bmcl.2010.08.070. Epub 2010 Aug 19. Bioorg Med Chem Lett. 2010. PMID: 20822903
Design, synthesis, and crystal structure of hydroxyethyl secondary amine-based peptidomimetic inhibitors of human beta-secretase.
Maillard MC, Hom RK, Benson TE, Moon JB, Mamo S, Bienkowski M, Tomasselli AG, Woods DD, Prince DB, Paddock DJ, Emmons TL, Tucker JA, Dappen MS, Brogley L, Thorsett ED, Jewett N, Sinha S, John V. Maillard MC, et al. Among authors: tucker ja. J Med Chem. 2007 Feb 22;50(4):776-81. doi: 10.1021/jm061242y. J Med Chem. 2007. PMID: 17300163
Design and synthesis of cell potent BACE-1 inhibitors: structure-activity relationship of P1' substituents.
Sealy JM, Truong AP, Tso L, Probst GD, Aquino J, Hom RK, Jagodzinska BM, Dressen D, Wone DW, Brogley L, John V, Tung JS, Pleiss MA, Tucker JA, Konradi AW, Dappen MS, Toth G, Pan H, Ruslim L, Miller J, Bova MP, Sinha S, Quinn KP, Sauer JM. Sealy JM, et al. Among authors: tucker ja. Bioorg Med Chem Lett. 2009 Nov 15;19(22):6386-91. doi: 10.1016/j.bmcl.2009.09.061. Epub 2009 Sep 19. Bioorg Med Chem Lett. 2009. PMID: 19811916
Improving the permeability of the hydroxyethylamine BACE-1 inhibitors: structure-activity relationship of P2' substituents.
Truong AP, Probst GD, Aquino J, Fang L, Brogley L, Sealy JM, Hom RK, Tucker JA, John V, Tung JS, Pleiss MA, Konradi AW, Sham HL, Dappen MS, Tóth G, Yao N, Brecht E, Pan H, Artis DR, Ruslim L, Bova MP, Sinha S, Yednock TA, Zmolek W, Quinn KP, Sauer JM. Truong AP, et al. Among authors: tucker ja. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4789-94. doi: 10.1016/j.bmcl.2010.06.112. Epub 2010 Jun 25. Bioorg Med Chem Lett. 2010. PMID: 20634069
Amyloid precursor protein selective gamma-secretase inhibitors for treatment of Alzheimer's disease.
Basi GS, Hemphill S, Brigham EF, Liao A, Aubele DL, Baker J, Barbour R, Bova M, Chen XH, Dappen MS, Eichenbaum T, Goldbach E, Hawkinson J, Lawler-Herbold R, Hu K, Hui T, Jagodzinski JJ, Keim PS, Kholodenko D, Latimer LH, Lee M, Marugg J, Mattson MN, McCauley S, Miller JL, Motter R, Mutter L, Neitzel ML, Ni H, Nguyen L, Quinn K, Ruslim L, Semko CM, Shapiro P, Smith J, Soriano F, Szoke B, Tanaka K, Tang P, Tucker JA, Ye XM, Yu M, Wu J, Xu YZ, Garofalo AW, Sauer JM, Konradi AW, Ness D, Shopp G, Pleiss MA, Freedman SB, Schenk D. Basi GS, et al. Among authors: tucker ja. Alzheimers Res Ther. 2010 Dec 29;2(6):36. doi: 10.1186/alzrt60. Alzheimers Res Ther. 2010. PMID: 21190552 Free PMC article.
Design and synthesis of human immunodeficiency virus entry inhibitors: sulfonamide as an isostere for the alpha-ketoamide group.
Lu RJ, Tucker JA, Zinevitch T, Kirichenko O, Konoplev V, Kuznetsova S, Sviridov S, Pickens J, Tandel S, Brahmachary E, Yang Y, Wang J, Freel S, Fisher S, Sullivan A, Zhou J, Stanfield-Oakley S, Greenberg M, Bolognesi D, Bray B, Koszalka B, Jeffs P, Khasanov A, Ma YA, Jeffries C, Liu C, Proskurina T, Zhu T, Chucholowski A, Li R, Sexton C. Lu RJ, et al. Among authors: tucker ja. J Med Chem. 2007 Dec 27;50(26):6535-44. doi: 10.1021/jm070650e. Epub 2007 Dec 4. J Med Chem. 2007. PMID: 18052117
Synthesis and biological activity of aminoguanidine and diaminoguanidine analogues of the antidiabetic/antiobesity agent 3-guanidinopropionic acid.
Vaillancourt VA, Larsen SD, Tanis SP, Burr JE, Connell MA, Cudahy MM, Evans BR, Fisher PV, May PD, Meglasson MD, Robinson DD, Stevens FC, Tucker JA, Vidmar TJ, Yu JH. Vaillancourt VA, et al. Among authors: tucker ja. J Med Chem. 2001 Apr 12;44(8):1231-48. doi: 10.1021/jm000094n. J Med Chem. 2001. PMID: 11312923
Synthesis and biological activity of analogues of the antidiabetic/antiobesity agent 3-guanidinopropionic acid: discovery of a novel aminoguanidinoacetic acid antidiabetic agent.
Larsen SD, Connell MA, Cudahy MM, Evans BR, May PD, Meglasson MD, O'Sullivan TJ, Schostarez HJ, Sih JC, Stevens FC, Tanis SP, Tegley CM, Tucker JA, Vaillancourt VA, Vidmar TJ, Watt W, Yu JH. Larsen SD, et al. Among authors: tucker ja. J Med Chem. 2001 Apr 12;44(8):1217-30. doi: 10.1021/jm000095f. J Med Chem. 2001. PMID: 11312922
330 results