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Page 1
Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2.
DiMauro EF, Buchanan JL, Cheng A, Emkey R, Hitchcock SA, Huang L, Huang MY, Janosky B, Lee JH, Li X, Martin MW, Tomlinson SA, White RD, Zheng XM, Patel VF, Fremeau RT Jr. DiMauro EF, et al. Among authors: hitchcock sa. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4267-74. doi: 10.1016/j.bmcl.2008.06.096. Epub 2008 Jul 3. Bioorg Med Chem Lett. 2008. PMID: 18640038
Discovery and optimization of a novel series of N-arylamide oxadiazoles as potent, highly selective and orally bioavailable cannabinoid receptor 2 (CB2) agonists.
Cheng Y, Albrecht BK, Brown J, Buchanan JL, Buckner WH, DiMauro EF, Emkey R, Fremeau RT Jr, Harmange JC, Hoffman BJ, Huang L, Huang M, Lee JH, Lin FF, Martin MW, Nguyen HQ, Patel VF, Tomlinson SA, White RD, Xia X, Hitchcock SA. Cheng Y, et al. Among authors: hitchcock sa. J Med Chem. 2008 Aug 28;51(16):5019-34. doi: 10.1021/jm800463f. Epub 2008 Aug 5. J Med Chem. 2008. PMID: 18680277
Hydroxyethylamine-based inhibitors of BACE1: P₁-P₃ macrocyclization can improve potency, selectivity, and cell activity.
Pennington LD, Whittington DA, Bartberger MD, Jordan SR, Monenschein H, Nguyen TT, Yang BH, Xue QM, Vounatsos F, Wahl RC, Chen K, Wood S, Citron M, Patel VF, Hitchcock SA, Zhong W. Pennington LD, et al. Among authors: hitchcock sa. Bioorg Med Chem Lett. 2013 Aug 1;23(15):4459-64. doi: 10.1016/j.bmcl.2013.05.028. Epub 2013 May 16. Bioorg Med Chem Lett. 2013. PMID: 23769639
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: hitchcock sa. 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
An Orally Available BACE1 Inhibitor That Affords Robust CNS Aβ Reduction without Cardiovascular Liabilities.
Cheng Y, Brown J, Judd TC, Lopez P, Qian W, Powers TS, Chen JJ, Bartberger MD, Chen K, Dunn RT 2nd, Epstein O, Fremeau RT Jr, Harried S, Hickman D, Hitchcock SA, Luo Y, Minatti AE, Patel VF, Vargas HM, Wahl RC, Weiss MM, Wen PH, White RD, Whittington DA, Zheng XM, Wood S. Cheng Y, et al. Among authors: hitchcock sa. ACS Med Chem Lett. 2014 Dec 29;6(2):210-5. doi: 10.1021/ml500458t. eCollection 2015 Feb 12. ACS Med Chem Lett. 2014. PMID: 25699151 Free PMC article.
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: hitchcock sa. 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: hitchcock sa. 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: hitchcock sa. J Med Chem. 2012 Nov 8;55(21):9025-44. doi: 10.1021/jm300118s. Epub 2012 Apr 18. J Med Chem. 2012. PMID: 22468684
29 results