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Items: 23

1.

The BACE-1 inhibitor CNP520 for prevention trials in Alzheimer's disease.

Neumann U, Ufer M, Jacobson LH, Rouzade-Dominguez ML, Huledal G, Kolly C, Lüönd RM, Machauer R, Veenstra SJ, Hurth K, Rueeger H, Tintelnot-Blomley M, Staufenbiel M, Shimshek DR, Perrot L, Frieauff W, Dubost V, Schiller H, Vogg B, Beltz K, Avrameas A, Kretz S, Pezous N, Rondeau JM, Beckmann N, Hartmann A, Vormfelde S, David OJ, Galli B, Ramos R, Graf A, Lopez Lopez C.

EMBO Mol Med. 2018 Sep 17. pii: e9316. doi: 10.15252/emmm.201809316. [Epub ahead of print]

2.

Discovery of amino-1,4-oxazines as potent BACE-1 inhibitors.

Veenstra SJ, Rueeger H, Voegtle M, Lueoend R, Holzer P, Hurth K, Tintelnot-Blomley M, Frederiksen M, Rondeau JM, Jacobson L, Staufenbiel M, Neumann U, Machauer R.

Bioorg Med Chem Lett. 2018 Jul 1;28(12):2195-2200. doi: 10.1016/j.bmcl.2018.05.003. Epub 2018 May 3.

PMID:
29764741
3.

A novel BACE inhibitor NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in APP transgenic mice.

Neumann U, Rueeger H, Machauer R, Veenstra SJ, Lueoend RM, Tintelnot-Blomley M, Laue G, Beltz K, Vogg B, Schmid P, Frieauff W, Shimshek DR, Staufenbiel M, Jacobson LH.

Mol Neurodegener. 2015 Sep 3;10:44. doi: 10.1186/s13024-015-0033-8.

4.

Structure based design, synthesis and SAR of cyclic hydroxyethylamine (HEA) BACE-1 inhibitors.

Rueeger H, Rondeau JM, McCarthy C, Möbitz H, Tintelnot-Blomley M, Neumann U, Desrayaud S.

Bioorg Med Chem Lett. 2011 Apr 1;21(7):1942-7. doi: 10.1016/j.bmcl.2011.02.038. Epub 2011 Feb 15.

PMID:
21388807
5.

Exploring subtype selectivity and metabolic stability of a novel series of ligands for the benzodiazepine binding site of the GABAA receptor.

Hintermann S, Hurth K, Nozulak J, Tintelnot-Blomley M, Aichholz R, Blanz J, Kaupmann K, Mosbacher J.

Bioorg Med Chem Lett. 2011 Mar 1;21(5):1523-6. doi: 10.1016/j.bmcl.2010.12.107. Epub 2010 Dec 28.

PMID:
21277199
6.

Substrate-controlled and organocatalytic asymmetric synthesis of carbocyclic amino acid dipeptide mimetics.

Hanessian S, Maji DK, Govindan S, Matera R, Tintelnot-Blomley M.

J Org Chem. 2010 May 7;75(9):2861-76. doi: 10.1021/jo100017t.

PMID:
20392053
7.

Structure-based design and synthesis of novel P2/P3 modified, non-peptidic beta-secretase (BACE-1) inhibitors.

Hanessian S, Shao Z, Betschart C, Rondeau JM, Neumann U, Tintelnot-Blomley M.

Bioorg Med Chem Lett. 2010 Mar 15;20(6):1924-7. doi: 10.1016/j.bmcl.2010.01.139. Epub 2010 Feb 2. Erratum in: Bioorg Med Chem Lett. 2013 Apr 15;23(8):2460-1.

PMID:
20172717
8.

Macrocyclic BACE-1 inhibitors acutely reduce Abeta in brain after po application.

Lerchner A, Machauer R, Betschart C, Veenstra S, Rueeger H, McCarthy C, Tintelnot-Blomley M, Jaton AL, Rabe S, Desrayaud S, Enz A, Staufenbiel M, Paganetti P, Rondeau JM, Neumann U.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):603-7. doi: 10.1016/j.bmcl.2009.11.092. Epub 2009 Nov 22.

PMID:
19963375
9.

Macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors with activity in vivo.

Machauer R, Laumen K, Veenstra S, Rondeau JM, Tintelnot-Blomley M, Betschart C, Jaton AL, Desrayaud S, Staufenbiel M, Rabe S, Paganetti P, Neumann U.

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1366-70. doi: 10.1016/j.bmcl.2009.01.055. Epub 2009 Jan 22.

PMID:
19195887
10.

Structure-based design and synthesis of macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors.

Machauer R, Veenstra S, Rondeau JM, Tintelnot-Blomley M, Betschart C, Neumann U, Paganetti P.

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1361-5. doi: 10.1016/j.bmcl.2009.01.036. Epub 2009 Jan 19. Erratum in: Bioorg Med Chem Lett. 2009 Apr 15;19(8):2366.

PMID:
19195886
11.

2-Cyano-pyrimidines: a new chemotype for inhibitors of the cysteine protease cathepsin K.

Altmann E, Aichholz R, Betschart C, Buhl T, Green J, Irie O, Teno N, Lattmann R, Tintelnot-Blomley M, Missbach M.

J Med Chem. 2007 Feb 22;50(4):591-4. Epub 2007 Jan 27.

PMID:
17256925
12.

Structure-based design and synthesis of macroheterocyclic peptidomimetic inhibitors of the aspartic protease beta-site amyloid precursor protein cleaving enzyme (BACE).

Hanessian S, Yang G, Rondeau JM, Neumann U, Betschart C, Tintelnot-Blomley M.

J Med Chem. 2006 Jul 27;49(15):4544-67.

PMID:
16854060
13.

A critical appraisal of structure-based drug design.

Tintelnot-Blomley M, Lewis RA.

IDrugs. 2006 Feb;9(2):114-8.

PMID:
16523401
16.

Structure-based design, synthesis, and memapsin 2 (BACE) inhibitory activity of carbocyclic and heterocyclic peptidomimetics.

Hanessian S, Yun H, Hou Y, Yang G, Bayrakdarian M, Therrien E, Moitessier N, Roggo S, Veenstra S, Tintelnot-Blomley M, Rondeau JM, Ostermeier C, Strauss A, Ramage P, Paganetti P, Neumann U, Betschart C.

J Med Chem. 2005 Aug 11;48(16):5175-90.

PMID:
16078837
17.

Cyclophilin D as a drug target.

Waldmeier PC, Zimmermann K, Qian T, Tintelnot-Blomley M, Lemasters JJ.

Curr Med Chem. 2003 Aug;10(16):1485-506. Review.

PMID:
12871122
18.

Arylaminoethyl amides as inhibitors of the cysteine protease cathepsin K-investigating P1' substituents.

Altmann E, Green J, Tintelnot-Blomley M.

Bioorg Med Chem Lett. 2003 Jun 16;13(12):1997-2001.

PMID:
12781182
19.

New aza-dipeptide analogues as potent and orally absorbed HIV-1 protease inhibitors: candidates for clinical development.

Bold G, Fässler A, Capraro HG, Cozens R, Klimkait T, Lazdins J, Mestan J, Poncioni B, Rösel J, Stover D, Tintelnot-Blomley M, Acemoglu F, Beck W, Boss E, Eschbach M, Hürlimann T, Masso E, Roussel S, Ucci-Stoll K, Wyss D, Lang M.

J Med Chem. 1998 Aug 27;41(18):3387-401.

PMID:
9719591
20.

Semicochliodinol A and B: inhibitors of HIV-1 protease and EGF-R protein tyrosine kinase related to asterriquinones produced by the fungus Chrysosporium merdarium.

Fredenhagen A, Petersen F, Tintelnot-Blomley M, Rösel J, Mett H, Hug P.

J Antibiot (Tokyo). 1997 May;50(5):395-401.

21.

Profile of CGP 61755: a novel and potent HIV-1 protease inhibitor that shows enhanced anti-HIV activity when combined with other antiretroviral agents in vitro.

Lazdins JK, Bold G, Capraro HG, Cozens R, Fässler A, Flesch G, Klimkait T, Lang M, Mestan J, Poncioni B, Rösel J, Stover D, Tintelnot-Blomley M, Walker MR, Woods-Cook K.

Schweiz Med Wochenschr. 1996 Oct 26;126(43):1849-51.

PMID:
8916294
22.

Aza-peptide analogs as potent human immunodeficiency virus type-1 protease inhibitors with oral bioavailability.

Fässler A, Bold G, Capraro HG, Cozens R, Mestan J, Poncioni B, Rösel J, Tintelnot-Blomley M, Lang M.

J Med Chem. 1996 Aug 2;39(16):3203-16.

PMID:
8759643
23.

Comparative analysis of the X-ray structures of HIV-1 and HIV-2 proteases in complex with CGP 53820, a novel pseudosymmetric inhibitor.

Priestle JP, Fässler A, Rösel J, Tintelnot-Blomley M, Strop P, Grütter MG.

Structure. 1995 Apr 15;3(4):381-9. Erratum in: Structure 1995 Jun 15;3(6):629.

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