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Items: 1 to 20 of 131

1.

Highly selective azadipeptide nitrile inhibitors for cathepsin K: design, synthesis and activity assays.

Ren XF, Li HW, Fang X, Wu Y, Wang L, Zou S.

Org Biomol Chem. 2013 Feb 21;11(7):1143-8. doi: 10.1039/c2ob26624e.

PMID:
23299878
2.

Highly selective aza-nitrile inhibitors for cathepsin K, structural optimization and molecular modeling.

Yuan XY, Fu DY, Ren XF, Fang X, Wang L, Zou S, Wu Y.

Org Biomol Chem. 2013 Sep 21;11(35):5847-52. doi: 10.1039/c3ob41165f.

PMID:
23900712
3.

Structural optimization of azadipeptide nitriles strongly increases association rates and allows the development of selective cathepsin inhibitors.

Frizler M, Lohr F, Furtmann N, Kläs J, Gütschow M.

J Med Chem. 2011 Jan 13;54(1):396-400. doi: 10.1021/jm101272p. Erratum in: J Med Chem. 2011 Jan 13;54(1):399.

PMID:
21128614
4.

Azadipeptide nitriles: highly potent and proteolytically stable inhibitors of papain-like cysteine proteases.

Löser R, Frizler M, Schilling K, Gütschow M.

Angew Chem Int Ed Engl. 2008;47(23):4331-4. doi: 10.1002/anie.200705858. No abstract available.

PMID:
18404765
5.

Dipeptide-derived nitriles containing additional electrophilic sites: potentially irreversible inhibitors of cysteine proteases.

Löser R, Gütschow M.

J Enzyme Inhib Med Chem. 2009 Dec;24(6):1245-52. doi: 10.3109/14756360902797328.

PMID:
19912058
6.

Fluorescent nitrile-based inhibitors of cysteine cathepsins.

Frizler M, Mertens MD, Gütschow M.

Bioorg Med Chem Lett. 2012 Dec 15;22(24):7715-8. doi: 10.1016/j.bmcl.2012.09.086.

PMID:
23122525
7.

Antimalarial activity of azadipeptide nitriles.

Löser R, Gut J, Rosenthal PJ, Frizler M, Gütschow M, Andrews KT.

Bioorg Med Chem Lett. 2010 Jan 1;20(1):252-5. doi: 10.1016/j.bmcl.2009.10.122.

8.

Development of N-(Functionalized benzoyl)-homocycloleucyl-glycinonitriles as Potent Cathepsin K Inhibitors.

Borišek J, Vizovišek M, Sosnowski P, Turk B, Turk D, Mohar B, Novič M.

J Med Chem. 2015 Sep 10;58(17):6928-37. doi: 10.1021/acs.jmedchem.5b00746.

PMID:
26280490
9.

Dipeptide nitrile inhibitors of cathepsin K.

Altmann E, Aichholz R, Betschart C, Buhl T, Green J, Lattmann R, Missbach M.

Bioorg Med Chem Lett. 2006 May 1;16(9):2549-54.

PMID:
16480867
10.

Novel, nonpeptidic cyanamides as potent and reversible inhibitors of human cathepsins K and L.

Falgueyret JP, Oballa RM, Okamoto O, Wesolowski G, Aubin Y, Rydzewski RM, Prasit P, Riendeau D, Rodan SB, Percival MD.

J Med Chem. 2001 Jan 4;44(1):94-104.

PMID:
11141092
11.

Selective nitrile inhibitors to modulate the proteolytic synergism of cathepsins S and F.

Frizler M, Schmitz J, Schulz-Fincke AC, Gütschow M.

J Med Chem. 2012 Jun 28;55(12):5982-6. doi: 10.1021/jm300734k.

PMID:
22686657
12.

Interaction of papain-like cysteine proteases with dipeptide-derived nitriles.

Löser R, Schilling K, Dimmig E, Gütschow M.

J Med Chem. 2005 Dec 1;48(24):7688-707.

PMID:
16302809
13.

Active Site Mapping of Human Cathepsin F with Dipeptide Nitrile Inhibitors.

Schmitz J, Furtmann N, Ponert M, Frizler M, Löser R, Bartz U, Bajorath J, Gütschow M.

ChemMedChem. 2015 Aug;10(8):1365-77. doi: 10.1002/cmdc.201500151.

PMID:
26119278
14.

Optimization of triazine nitriles as rhodesain inhibitors: structure-activity relationships, bioisosteric imidazopyridine nitriles, and X-ray crystal structure analysis with human cathepsin L.

Ehmke V, Winkler E, Banner DW, Haap W, Schweizer WB, Rottmann M, Kaiser M, Freymond C, Schirmeister T, Diederich F.

ChemMedChem. 2013 Jun;8(6):967-75. doi: 10.1002/cmdc.201300112.

PMID:
23658062
15.

Novel purine nitrile derived inhibitors of the cysteine protease cathepsin K.

Altmann E, Cowan-Jacob SW, Missbach M.

J Med Chem. 2004 Nov 18;47(24):5833-6.

PMID:
15537340
16.

Dioxo-triazines as a novel series of cathepsin K inhibitors.

Rankovic Z, Cai J, Fradera X, Dempster M, Mistry A, Mitchell A, Long C, Hamilton E, King A, Boucharens S, Jamieson C, Gillespie J, Cumming I, Uitdehaag J, van Zeeland M.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1488-90. doi: 10.1016/j.bmcl.2010.01.116.

PMID:
20153187
17.

Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases.

Wieczerzak E, Drabik P, Łankiewicz L, Ołdziej S, Grzonka Z, Abrahamson M, Grubb A, Brömme D.

J Med Chem. 2002 Sep 12;45(19):4202-11.

PMID:
12213061
18.

5-Aminopyrimidin-2-ylnitriles as cathepsin K inhibitors.

Morley AD, Kenny PW, Burton B, Heald RA, Macfaul PA, Mullett J, Page K, Porres SS, Ribeiro LR, Smith P, Ward S, Wilkinson TJ.

Bioorg Med Chem Lett. 2009 Mar 15;19(6):1658-61. doi: 10.1016/j.bmcl.2009.01.110.

PMID:
19231183
19.

Design and synthesis of dipeptide nitriles as reversible and potent Cathepsin S inhibitors.

Ward YD, Thomson DS, Frye LL, Cywin CL, Morwick T, Emmanuel MJ, Zindell R, McNeil D, Bekkali Y, Girardot M, Hrapchak M, DeTuri M, Crane K, White D, Pav S, Wang Y, Hao MH, Grygon CA, Labadia ME, Freeman DM, Davidson W, Hopkins JL, Brown ML, Spero DM.

J Med Chem. 2002 Dec 5;45(25):5471-82. Erratum in: J Med Chem. 2003 Feb 27;46(5):882.. Giradot Marc [corrected to Girardot Marc].

PMID:
12459015
20.

A novel class of nonpeptidic biaryl inhibitors of human cathepsin K.

Robichaud J, Oballa R, Prasit P, Falgueyret JP, Percival MD, Wesolowski G, Rodan SB, Kimmel D, Johnson C, Bryant C, Venkatraman S, Setti E, Mendonca R, Palmer JT.

J Med Chem. 2003 Aug 14;46(17):3709-27.

PMID:
12904076
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