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Items: 1 to 20 of 175

1.

Structure based design of iminohydantoin BACE1 inhibitors: identification of an orally available, centrally active BACE1 inhibitor.

Cumming JN, Smith EM, Wang L, Misiaszek J, Durkin J, Pan J, Iserloh U, Wu Y, Zhu Z, Strickland C, Voigt J, Chen X, Kennedy ME, Kuvelkar R, Hyde LA, Cox K, Favreau L, Czarniecki MF, Greenlee WJ, McKittrick BA, Parker EM, Stamford AW.

Bioorg Med Chem Lett. 2012 Apr 1;22(7):2444-9. doi: 10.1016/j.bmcl.2012.02.013. Epub 2012 Feb 16.

PMID:
22390835
2.

Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor.

May PC, Dean RA, Lowe SL, Martenyi F, Sheehan SM, Boggs LN, Monk SA, Mathes BM, Mergott DJ, Watson BM, Stout SL, Timm DE, Smith Labell E, Gonzales CR, Nakano M, Jhee SS, Yen M, Ereshefsky L, Lindstrom TD, Calligaro DO, Cocke PJ, Greg Hall D, Friedrich S, Citron M, Audia JE.

J Neurosci. 2011 Nov 16;31(46):16507-16. doi: 10.1523/JNEUROSCI.3647-11.2011.

3.

Pyridinyl aminohydantoins as small molecule BACE1 inhibitors.

Zhou P, Li Y, Fan Y, Wang Z, Chopra R, Olland A, Hu Y, Magolda RL, Pangalos M, Reinhart PH, Turner MJ, Bard J, Malamas MS, Robichaud AJ.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2326-9. doi: 10.1016/j.bmcl.2010.01.136. Epub 2010 Feb 12.

PMID:
20202842
4.

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.

J Med Chem. 2011 Aug 25;54(16):5836-57. doi: 10.1021/jm200544q. Epub 2011 Jul 29.

PMID:
21707077
5.

Establishing the relationship between in vitro potency, pharmacokinetic, and pharmacodynamic parameters in a series of orally available, hydroxyethylamine-derived β-secretase inhibitors.

Wood S, Wen PH, Zhang J, Zhu L, Luo Y, Babu-Khan S, Chen K, Pham R, Esmay J, Dineen TA, Kaller MR, Weiss MM, Hitchcock SA, Citron M, Zhong W, Hickman D, Williamson T.

J Pharmacol Exp Ther. 2012 Nov;343(2):460-7. doi: 10.1124/jpet.112.197954. Epub 2012 Aug 21.

6.

Discovery of cyclic sulfoxide hydroxyethylamines as potent and selective β-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure based design and in vivo reduction of amyloid β-peptides.

Rueeger H, Lueoend R, Machauer R, Veenstra SJ, Jacobson LH, Staufenbiel M, Desrayaud S, Rondeau JM, Möbitz H, Neumann U.

Bioorg Med Chem Lett. 2013 Oct 1;23(19):5300-6. doi: 10.1016/j.bmcl.2013.07.071. Epub 2013 Aug 9.

PMID:
23981898
7.

Piperazine sulfonamide BACE1 inhibitors: design, synthesis, and in vivo characterization.

Cumming J, Babu S, Huang Y, Carrol C, Chen X, Favreau L, Greenlee W, Guo T, Kennedy M, Kuvelkar R, Le T, Li G, McHugh N, Orth P, Ozgur L, Parker E, Saionz K, Stamford A, Strickland C, Tadesse D, Voigt J, Zhang L, Zhang Q.

Bioorg Med Chem Lett. 2010 May 1;20(9):2837-42. doi: 10.1016/j.bmcl.2010.03.050. Epub 2010 Mar 12.

PMID:
20347593
8.

New pyrazolyl and thienyl aminohydantoins as potent BACE1 inhibitors: exploring the S2' region.

Malamas MS, Erdei J, Gunawan I, Barnes K, Hui Y, Johnson M, Robichaud A, Zhou P, Yan Y, Solvibile W, Turner J, Fan KY, Chopra R, Bard J, Pangalos MN.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5164-70. doi: 10.1016/j.bmcl.2011.07.057. Epub 2011 Jul 23.

PMID:
21835615
9.

Discovery and initial optimization of 5,5'-disubstituted aminohydantoins as potent beta-secretase (BACE1) inhibitors.

Nowak P, Cole DC, Aulabaugh A, Bard J, Chopra R, Cowling R, Fan KY, Hu B, Jacobsen S, Jani M, Jin G, Lo MC, Malamas MS, Manas ES, Narasimhan R, Reinhart P, Robichaud AJ, Stock JR, Subrath J, Svenson K, Turner J, Wagner E, Zhou P, Ellingboe JW.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):632-5. doi: 10.1016/j.bmcl.2009.11.052. Epub 2009 Nov 20.

PMID:
19959359
10.

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.

J Med Chem. 2012 Nov 8;55(21):9025-44. doi: 10.1021/jm300118s. Epub 2012 Apr 18.

PMID:
22468684
11.

Structure- and property-based design of aminooxazoline xanthenes as selective, orally efficacious, and CNS penetrable BACE inhibitors for the treatment of Alzheimer's disease.

Huang H, La DS, Cheng AC, Whittington DA, Patel VF, Chen K, Dineen TA, Epstein O, Graceffa R, Hickman D, Kiang YH, Louie S, Luo Y, Wahl RC, Wen PH, Wood S, Fremeau RT Jr.

J Med Chem. 2012 Nov 8;55(21):9156-69. doi: 10.1021/jm300598e. Epub 2012 Sep 11.

PMID:
22928914
12.

The selective BACE1 inhibitor VIa reduces amyloid-β production in cell and mouse models of Alzheimer's disease.

Cheng X, Zhou Y, Gu W, Wu J, Nie A, Cheng J, Zhou J, Zhou W, Zhang Y.

J Alzheimers Dis. 2013;37(4):823-34. doi: 10.3233/JAD-130836.

PMID:
23948917
13.

Oral administration of a potent and selective non-peptidic BACE-1 inhibitor decreases beta-cleavage of amyloid precursor protein and amyloid-beta production in vivo.

Hussain I, Hawkins J, Harrison D, Hille C, Wayne G, Cutler L, Buck T, Walter D, Demont E, Howes C, Naylor A, Jeffrey P, Gonzalez MI, Dingwall C, Michel A, Redshaw S, Davis JB.

J Neurochem. 2007 Feb;100(3):802-9.

14.

Synthesis and evaluation of arylquinones as BACE1 inhibitors, β-amyloid peptide aggregation inhibitors, and destabilizers of preformed β-amyloid fibrils.

Ortega A, Rincón Á, Jiménez-Aliaga KL, Bermejo-Bescós P, Martín-Aragón S, Molina MT, Csákÿ AG.

Bioorg Med Chem Lett. 2011 Apr 15;21(8):2183-7. doi: 10.1016/j.bmcl.2011.03.023. Epub 2011 Mar 13.

PMID:
21441028
15.

Tripeptidic BACE1 inhibitors devised by in-silico conformational structure-based design.

Hamada Y, Tagad HD, Nishimura Y, Ishiura S, Kiso Y.

Bioorg Med Chem Lett. 2012 Jan 15;22(2):1130-5. doi: 10.1016/j.bmcl.2011.11.102. Epub 2011 Dec 1.

PMID:
22178553
16.

Discovery of a series of efficient, centrally efficacious BACE1 inhibitors through structure-based drug design.

Butler CR, Brodney MA, Beck EM, Barreiro G, Nolan CE, Pan F, Vajdos F, Parris K, Varghese AH, Helal CJ, Lira R, Doran SD, Riddell DR, Buzon LM, Dutra JK, Martinez-Alsina LA, Ogilvie K, Murray JC, Young JM, Atchison K, Robshaw A, Gonzales C, Wang J, Zhang Y, O'Neill BT.

J Med Chem. 2015 Mar 26;58(6):2678-702. doi: 10.1021/jm501833t. Epub 2015 Mar 9.

PMID:
25695670
17.

A therapeutic antibody targeting BACE1 inhibits amyloid-β production in vivo.

Atwal JK, Chen Y, Chiu C, Mortensen DL, Meilandt WJ, Liu Y, Heise CE, Hoyte K, Luk W, Lu Y, Peng K, Wu P, Rouge L, Zhang Y, Lazarus RA, Scearce-Levie K, Wang W, Wu Y, Tessier-Lavigne M, Watts RJ.

Sci Transl Med. 2011 May 25;3(84):84ra43. doi: 10.1126/scitranslmed.3002254.

18.

Population PKPD modeling of BACE1 inhibitor-induced reduction in Aβ levels in vivo and correlation to in vitro potency in primary cortical neurons from mouse and guinea pig.

Janson J, Eketjäll S, Tunblad K, Jeppsson F, Von Berg S, Niva C, Radesäter AC, Fälting J, Visser SA.

Pharm Res. 2014 Mar;31(3):670-83. doi: 10.1007/s11095-013-1189-y. Epub 2013 Oct 3.

PMID:
24092053
19.

Thiophene substituted acylguanidines as BACE1 inhibitors.

Fobare WF, Solvibile WR, Robichaud AJ, Malamas MS, Manas E, Turner J, Hu Y, Wagner E, Chopra R, Cowling R, Jin G, Bard J.

Bioorg Med Chem Lett. 2007 Oct 1;17(19):5353-6. Epub 2007 Aug 11.

PMID:
17761418
20.

Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors.

Thompson LA, Shi J, Decicco CP, Tebben AJ, Olson RE, Boy KM, Guernon JM, Good AC, Liauw A, Zheng C, Copeland RA, Combs AP, Trainor GL, Camac DM, Muckelbauer JK, Lentz KA, Grace JE, Burton CR, Toyn JH, Barten DM, Marcinkeviciene J, Meredith JE, Albright CF, Macor JE.

Bioorg Med Chem Lett. 2011 Nov 15;21(22):6909-15. doi: 10.1016/j.bmcl.2011.06.116. Epub 2011 Jul 2.

PMID:
21974952

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