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Items: 1 to 20 of 134

1.

Structure-activity relationship study of BACE1 inhibitors possessing a chelidonic or 2,6-pyridinedicarboxylic scaffold at the P(2) position.

Hamada Y, Suzuki K, Nakanishi T, Sarma D, Ohta H, Yamaguchi R, Yamasaki M, Hidaka K, Ishiura S, Kiso Y.

Bioorg Med Chem Lett. 2014 Jan 15;24(2):618-23. doi: 10.1016/j.bmcl.2013.12.007. Epub 2013 Dec 8.

PMID:
24360554
2.

Significance of interactions of BACE1-Arg235 with its ligands and design of BACE1 inhibitors with P2 pyridine scaffold.

Hamada Y, Ohta H, Miyamoto N, Sarma D, Hamada T, Nakanishi T, Yamasaki M, Yamani A, Ishiura S, Kiso Y.

Bioorg Med Chem Lett. 2009 May 1;19(9):2435-9. doi: 10.1016/j.bmcl.2009.03.049. Epub 2009 Mar 18. Erratum in: Bioorg Med Chem Lett. 2009 Aig 1;19(15):4515.

PMID:
19345096
3.

Novel BACE1 inhibitors possessing a 5-nitroisophthalic scaffold at the P2 position.

Hamada Y, Nakanishi T, Suzuki K, Yamaguchi R, Hamada T, Hidaka K, Ishiura S, Kiso Y.

Bioorg Med Chem Lett. 2012 Jul 15;22(14):4640-4. doi: 10.1016/j.bmcl.2012.05.089. Epub 2012 Jun 1.

PMID:
22726930
4.

Novel non-peptidic and small-sized BACE1 inhibitors.

Hamada Y, Ohta H, Miyamoto N, Yamaguchi R, Yamani A, Hidaka K, Kimura T, Saito K, Hayashi Y, Ishiura S, Kiso Y.

Bioorg Med Chem Lett. 2008 Mar 1;18(5):1643-7. doi: 10.1016/j.bmcl.2008.01.056. Epub 2008 Jan 19.

PMID:
18261904
5.

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
6.

Structure-guided design and synthesis of P1' position 1-phenylcycloalkylamine-derived pentapeptidic BACE1 inhibitors.

Tagad HD, Hamada Y, Nguyen JT, Hidaka K, Hamada T, Sohma Y, Kimura T, Kiso Y.

Bioorg Med Chem. 2011 Sep 1;19(17):5238-46. doi: 10.1016/j.bmc.2011.07.002. Epub 2011 Jul 13.

PMID:
21803585
7.

Design of pentapeptidic BACE1 inhibitors with carboxylic acid bioisosteres at P1' and P4 positions.

Tagad HD, Hamada Y, Nguyen JT, Hamada T, Abdel-Rahman H, Yamani A, Nagamine A, Ikari H, Igawa N, Hidaka K, Sohma Y, Kimura T, Kiso Y.

Bioorg Med Chem. 2010 May 1;18(9):3175-86. doi: 10.1016/j.bmc.2010.03.032. Epub 2010 Mar 21.

PMID:
20381362
8.

Novel BACE1 inhibitors with a non-acidic heterocycle at the P1' position.

Suzuki K, Hamada Y, Nguyen JT, Kiso Y.

Bioorg Med Chem. 2013 Nov 1;21(21):6665-73. doi: 10.1016/j.bmc.2013.08.016. Epub 2013 Aug 12.

PMID:
23993670
9.

BACE1 inhibitors: optimization by replacing the P1' residue with non-acidic moiety.

Hamada Y, Abdel-Rahman H, Yamani A, Nguyen JT, Stochaj M, Hidaka K, Kimura T, Hayashi Y, Saito K, Ishiura S, Kiso Y.

Bioorg Med Chem Lett. 2008 Mar 1;18(5):1649-53. doi: 10.1016/j.bmcl.2008.01.058. Epub 2008 Jan 19.

PMID:
18249539
10.

KMI-358 and KMI-370, highly potent and small-sized BACE1 inhibitors containing phenylnorstatine.

Kimura T, Shuto D, Kasai S, Liu P, Hidaka K, Hamada T, Hayashi Y, Hattori C, Asai M, Kitazume S, Saido TC, Ishiura S, Kiso Y.

Bioorg Med Chem Lett. 2004 Mar 22;14(6):1527-31.

PMID:
15006396
11.

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.

12.

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
13.

A stereoselective approach to peptidomimetic BACE1 inhibitors.

Butini S, Gabellieri E, Brindisi M, Giovani S, Maramai S, Kshirsagar G, Guarino E, Brogi S, La Pietra V, Giustiniano M, Marinelli L, Novellino E, Campiani G, Cappelli A, Gemma S.

Eur J Med Chem. 2013;70:233-47. doi: 10.1016/j.ejmech.2013.09.056. Epub 2013 Oct 6.

PMID:
24158015
14.

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
15.

Virtual screening and structure-based discovery of indole acylguanidines as potent β-secretase (BACE1) inhibitors.

Zou Y, Li L, Chen W, Chen T, Ma L, Wang X, Xiong B, Xu Y, Shen J.

Molecules. 2013 May 16;18(5):5706-22. doi: 10.3390/molecules18055706.

16.

Carbazole-containing arylcarboxamides as BACE1 inhibitors.

Bertini S, Asso V, Ghilardi E, Granchi C, Manera C, Minutolo F, Saccomanni G, Bortolato A, Mason J, Moro S, Macchia M.

Bioorg Med Chem Lett. 2011 Nov 15;21(22):6657-61. doi: 10.1016/j.bmcl.2011.09.064. Epub 2011 Sep 21.

PMID:
21986588
17.

P-glycoprotein efflux and other factors limit brain amyloid beta reduction by beta-site amyloid precursor protein-cleaving enzyme 1 inhibitors in mice.

Meredith JE Jr, Thompson LA, Toyn JH, Marcin L, Barten DM, Marcinkeviciene J, Kopcho L, Kim Y, Lin A, Guss V, Burton C, Iben L, Polson C, Cantone J, Ford M, Drexler D, Fiedler T, Lentz KA, Grace JE Jr, Kolb J, Corsa J, Pierdomenico M, Jones K, Olson RE, Macor JE, Albright CF.

J Pharmacol Exp Ther. 2008 Aug;326(2):502-13. doi: 10.1124/jpet.108.138974. Epub 2008 May 22.

18.

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
19.

Inhibition of beta-secretase in vivo via antibody binding to unique loops (D and F) of BACE1.

Zhou L, Chávez-Gutiérrez L, Bockstael K, Sannerud R, Annaert W, May PC, Karran E, De Strooper B.

J Biol Chem. 2011 Mar 11;286(10):8677-87. doi: 10.1074/jbc.M110.194860. Epub 2011 Jan 5.

20.

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

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