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260 results

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Page 1
2-amino-1,3-thiazol-4(5H)-ones as potent and selective 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: enzyme-ligand co-crystal structure and demonstration of pharmacodynamic effects in C57Bl/6 mice.
Johansson L, Fotsch C, Bartberger MD, Castro VM, Chen M, Emery M, Gustafsson S, Hale C, Hickman D, Homan E, Jordan SR, Komorowski R, Li A, McRae K, Moniz G, Matsumoto G, Orihuela C, Palm G, Veniant M, Wang M, Williams M, Zhang J. Johansson L, et al. Among authors: hickman d. J Med Chem. 2008 May 22;51(10):2933-43. doi: 10.1021/jm701551j. Epub 2008 Apr 18. J Med Chem. 2008. PMID: 18419108
Further studies with the 2-amino-1,3-thiazol-4(5H)-one class of 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: reducing pregnane X receptor activity and exploring activity in a monkey pharmacodynamic model.
Fotsch C, Bartberger MD, Bercot EA, Chen M, Cupples R, Emery M, Fretland J, Guram A, Hale C, Han N, Hickman D, Hungate RW, Hayashi M, Komorowski R, Liu Q, Matsumoto G, St Jean DJ Jr, Ursu S, Véniant M, Xu G, Ye Q, Yuan C, Zhang J, Zhang X, Tu H, Wang M. Fotsch C, et al. Among authors: hickman d. J Med Chem. 2008 Dec 25;51(24):7953-67. doi: 10.1021/jm801073z. J Med Chem. 2008. PMID: 19053753
From fragment screening to in vivo efficacy: optimization of a series of 2-aminoquinolines as potent inhibitors of beta-site amyloid precursor protein cleaving enzyme 1 (BACE1).
Cheng Y, Judd TC, Bartberger MD, Brown J, Chen K, Fremeau RT Jr, Hickman D, Hitchcock SA, Jordan B, Li V, Lopez P, Louie SW, Luo Y, Michelsen K, Nixey T, Powers TS, Rattan C, Sickmier EA, St Jean DJ Jr, Wahl RC, Wen PH, Wood S. Cheng Y, et al. Among authors: hickman d. J Med Chem. 2011 Aug 25;54(16):5836-57. doi: 10.1021/jm200544q. Epub 2011 Jul 29. J Med Chem. 2011. PMID: 21707077
Design and preparation of a potent series of hydroxyethylamine containing β-secretase inhibitors that demonstrate robust reduction of central β-amyloid.
Weiss MM, Williamson T, Babu-Khan S, Bartberger MD, Brown J, Chen K, Cheng Y, Citron M, Croghan MD, Dineen TA, Esmay J, Graceffa RF, Harried SS, Hickman D, Hitchcock SA, Horne DB, Huang H, Imbeah-Ampiah R, Judd T, Kaller MR, Kreiman CR, La DS, Li V, Lopez P, Louie S, Monenschein H, Nguyen TT, Pennington LD, Rattan C, San Miguel T, Sickmier EA, Wahl RC, Wen PH, Wood S, Xue Q, Yang BH, Patel VF, Zhong W. Weiss MM, et al. Among authors: hickman d. J Med Chem. 2012 Nov 8;55(21):9009-24. doi: 10.1021/jm300119p. Epub 2012 Apr 18. J Med Chem. 2012. PMID: 22468639
Design and synthesis of potent, orally efficacious hydroxyethylamine derived β-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors.
Dineen TA, Weiss MM, Williamson T, Acton P, Babu-Khan S, Bartberger MD, Brown J, Chen K, Cheng Y, Citron M, Croghan MD, Dunn RT 2nd, Esmay J, Graceffa RF, Harried SS, Hickman D, Hitchcock SA, Horne DB, Huang H, Imbeah-Ampiah R, Judd T, Kaller MR, Kreiman CR, La DS, Li V, Lopez P, Louie S, Monenschein H, Nguyen TT, Pennington LD, San Miguel T, Sickmier EA, Vargas HM, Wahl RC, Wen PH, Whittington DA, Wood S, Xue Q, Yang BH, Patel VF, Zhong W. Dineen TA, et al. Among authors: hickman d. J Med Chem. 2012 Nov 8;55(21):9025-44. doi: 10.1021/jm300118s. Epub 2012 Apr 18. J Med Chem. 2012. PMID: 22468684
The development of a structurally distinct series of BACE1 inhibitors via the (Z)-fluoro-olefin amide bioisosteric replacement.
Frohn M, Liu L, Siegmund AC, Qian W, Amegadzie A, Chen N, Tan H, Hickman D, Wood S, Wen PH, Bartberger MD, Whittington DA, Allen JR, Bourbeau MP. Frohn M, et al. Among authors: hickman d. Bioorg Med Chem Lett. 2020 Jul 15;30(14):127240. doi: 10.1016/j.bmcl.2020.127240. Epub 2020 May 4. Bioorg Med Chem Lett. 2020. PMID: 32527542
Discovery of AM-6494: A Potent and Orally Efficacious β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor with in Vivo Selectivity over BACE2.
Pettus LH, Bourbeau MP, Bradley J, Bartberger MD, Chen K, Hickman D, Johnson M, Liu Q, Manning JR, Nanez A, Siegmund AC, Wen PH, Whittington DA, Allen JR, Wood S. Pettus LH, et al. Among authors: hickman d. J Med Chem. 2020 Mar 12;63(5):2263-2281. doi: 10.1021/acs.jmedchem.9b01034. Epub 2019 Oct 18. J Med Chem. 2020. PMID: 31589043
The optimization of aminooxadiazoles as orally active inhibitors of Cdc7.
Harrington PE, Bourbeau MP, Fotsch C, Frohn M, Pickrell AJ, Reichelt A, Sham K, Siegmund AC, Bailis JM, Bush T, Escobar S, Hickman D, Heller S, Hsieh F, Orf JN, Rong M, San Miguel T, Tan H, Zalameda L, Allen JG. Harrington PE, et al. Among authors: hickman d. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6396-400. doi: 10.1016/j.bmcl.2013.09.055. Epub 2013 Sep 25. Bioorg Med Chem Lett. 2013. PMID: 24120542
Development of 2-aminooxazoline 3-azaxanthenes as orally efficacious β-secretase inhibitors for the potential treatment of Alzheimer's disease.
Chen JJ, Liu Q, Yuan C, Gore V, Lopez P, Ma V, Amegadzie A, Qian W, Judd TC, Minatti AE, Brown J, Cheng Y, Xue M, Zhong W, Dineen TA, Epstein O, Human J, Kreiman C, Marx I, Weiss MM, Hitchcock SA, Powers TS, Chen K, Wen PH, Whittington DA, Cheng AC, Bartberger MD, Hickman D, Werner JA, Vargas HM, Everds NE, Vonderfecht SL, Dunn RT 2nd, Wood S, Fremeau RT Jr, White RD, Patel VF. Chen JJ, et al. Among authors: hickman d. Bioorg Med Chem Lett. 2015 Feb 15;25(4):767-74. doi: 10.1016/j.bmcl.2014.12.092. Epub 2015 Jan 8. Bioorg Med Chem Lett. 2015. PMID: 25613679
260 results