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Items: 1 to 20 of 128

1.

Design, synthesis, and qualitative structure-activity evaluations of novel β-secretase inhibitors as potential Alzheimer's drug leads.

Al-Tel TH, Semreen MH, Al-Qawasmeh RA, Schmidt MF, El-Awadi R, Ardah M, Zaarour R, Rao SN, El-Agnaf O.

J Med Chem. 2011 Dec 22;54(24):8373-85. doi: 10.1021/jm201181f. Epub 2011 Nov 16.

PMID:
22044119
2.

Di-substituted pyridinyl aminohydantoins as potent and highly selective human beta-secretase (BACE1) inhibitors.

Malamas MS, Barnes K, Johnson M, Hui Y, Zhou P, Turner J, Hu Y, Wagner E, Fan K, Chopra R, Olland A, Bard J, Pangalos M, Reinhart P, Robichaud AJ.

Bioorg Med Chem. 2010 Jan 15;18(2):630-9. doi: 10.1016/j.bmc.2009.12.007. Epub 2009 Dec 6.

PMID:
20045648
3.

Aminoimidazoles as potent and selective human beta-secretase (BACE1) inhibitors.

Malamas MS, Erdei J, Gunawan I, Barnes K, Johnson M, Hui Y, Turner J, Hu Y, Wagner E, Fan K, Olland A, Bard J, Robichaud AJ.

J Med Chem. 2009 Oct 22;52(20):6314-23. doi: 10.1021/jm9006752. Erratum in: J Med Chem. 2010 Feb 25;53(4):1882.

PMID:
19757823
4.

Design, synthesis and SAR analysis of potent BACE1 inhibitors: Possible lead drug candidates for Alzheimer's disease.

Tarazi H, Odeh RA, Al-Qawasmeh R, Yousef IA, Voelter W, Al-Tel TH.

Eur J Med Chem. 2017 Jan 5;125:1213-1224. doi: 10.1016/j.ejmech.2016.11.021. Epub 2016 Nov 12.

PMID:
27871037
5.

Design and synthesis of 5,5'-disubstituted aminohydantoins as potent and selective human beta-secretase (BACE1) inhibitors.

Malamas MS, Erdei J, Gunawan I, Turner J, Hu Y, Wagner E, Fan K, Chopra R, Olland A, Bard J, Jacobsen S, Magolda RL, Pangalos M, Robichaud AJ.

J Med Chem. 2010 Feb 11;53(3):1146-58. doi: 10.1021/jm901414e.

PMID:
19968289
6.

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
7.

Discovery of imidazopyridines containing isoindoline-1,3-dione framework as a new class of BACE1 inhibitors: Design, synthesis and SAR analysis.

Azimi S, Zonouzi A, Firuzi O, Iraji A, Saeedi M, Mahdavi M, Edraki N.

Eur J Med Chem. 2017 Sep 29;138:729-737. doi: 10.1016/j.ejmech.2017.06.040. Epub 2017 Jun 24.

PMID:
28728105
8.

Design, synthesis, and X-ray structure of potent memapsin 2 (beta-secretase) inhibitors with isophthalamide derivatives as the P2-P3-ligands.

Ghosh AK, Kumaragurubaran N, Hong L, Kulkarni SS, Xu X, Chang W, Weerasena V, Turner R, Koelsch G, Bilcer G, Tang J.

J Med Chem. 2007 May 17;50(10):2399-407. Epub 2007 Apr 14.

PMID:
17432843
9.

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
10.

Tetrapeptides, as small-sized peptidic inhibitors; synthesis and their inhibitory activity against BACE1.

Kakizawa T, Hidaka K, Hamada D, Yamaguchi R, Uemura T, Kitamura H, Tagad HD, Hamada T, Ziora Z, Hamada Y, Kimura T, Kiso Y.

J Pept Sci. 2010 Jun;16(6):257-62. doi: 10.1002/psc.1238.

PMID:
20474036
11.

Discovery of biphenylacetamide-derived inhibitors of BACE1 using de novo structure-based molecular design.

Mok NY, Chadwick J, Kellett KA, Casas-Arce E, Hooper NM, Johnson AP, Fishwick CW.

J Med Chem. 2013 Mar 14;56(5):1843-52. doi: 10.1021/jm301127x. Epub 2013 Feb 22.

PMID:
23374014
12.

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
13.

Application of fragment-based lead generation to the discovery of novel, cyclic amidine beta-secretase inhibitors with nanomolar potency, cellular activity, and high ligand efficiency.

Edwards PD, Albert JS, Sylvester M, Aharony D, Andisik D, Callaghan O, Campbell JB, Carr RA, Chessari G, Congreve M, Frederickson M, Folmer RH, Geschwindner S, Koether G, Kolmodin K, Krumrine J, Mauger RC, Murray CW, Olsson LL, Patel S, Spear N, Tian G.

J Med Chem. 2007 Nov 29;50(24):5912-25. Epub 2007 Nov 7.

PMID:
17985862
14.

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.

15.

Measuring human beta-secretase (BACE1) activity using homogeneous time-resolved fluorescence.

Kennedy ME, Wang W, Song L, Lee J, Zhang L, Wong G, Wang L, Parker E.

Anal Biochem. 2003 Aug 1;319(1):49-55.

PMID:
12842106
16.

Novel pyrrolyl 2-aminopyridines as potent and selective human beta-secretase (BACE1) inhibitors.

Malamas MS, Barnes K, Hui Y, Johnson M, Lovering F, Condon J, Fobare W, Solvibile W, Turner J, Hu Y, Manas ES, Fan K, Olland A, Chopra R, Bard J, Pangalos MN, Reinhart P, Robichaud AJ.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2068-73. doi: 10.1016/j.bmcl.2010.02.075. Epub 2010 Feb 23.

PMID:
20223661
17.

Is BACE1 a suitable therapeutic target for the treatment of Alzheimer's disease? Current strategies and future directions.

Klaver DW, Wilce MC, Cui H, Hung AC, Gasperini R, Foa L, Small DH.

Biol Chem. 2010 Aug;391(8):849-59. doi: 10.1515/BC.2010.089. Review.

PMID:
20731541
18.

Beta-secretase (BACE) as a drug target for Alzheimer's disease.

Vassar R.

Adv Drug Deliv Rev. 2002 Dec 7;54(12):1589-602. Review.

PMID:
12453676
19.

Design and synthesis of novel imidazole-substituted dipeptide amides as potent and selective inhibitors of Candida albicans myristoylCoA:protein N-myristoyltransferase and identification of related tripeptide inhibitors with mechanism-based antifungal activity.

Devadas B, Freeman SK, Zupec ME, Lu HF, Nagarajan SR, Kishore NS, Lodge JK, Kuneman DW, McWherter CA, Vinjamoori DV, Getman DP, Gordon JI, Sikorski JA.

J Med Chem. 1997 Aug 1;40(16):2609-25.

PMID:
9258368
20.

Discovery of a novel warhead against beta-secretase through fragment-based lead generation.

Geschwindner S, Olsson LL, Albert JS, Deinum J, Edwards PD, de Beer T, Folmer RH.

J Med Chem. 2007 Nov 29;50(24):5903-11. Epub 2007 Nov 7.

PMID:
17985861

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