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Items: 1 to 20 of 100

1.

Vinyl sulfone-based peptidomimetics as anti-trypanosomal agents: design, synthesis, biological and computational evaluation.

Dunny E, Doherty W, Evans P, Malthouse JP, Nolan D, Knox AJ.

J Med Chem. 2013 Sep 12;56(17):6638-50. doi: 10.1021/jm400294w. Epub 2013 Sep 3.

PMID:
23952916
2.

Design, synthesis and biological evaluation of potent azadipeptide nitrile inhibitors and activity-based probes as promising anti-Trypanosoma brucei agents.

Yang PY, Wang M, Li L, Wu H, He CY, Yao SQ.

Chemistry. 2012 May 21;18(21):6528-41. doi: 10.1002/chem.201103322. Epub 2012 Apr 4.

PMID:
22488888
3.

Preparation, anti-trypanosomal activity and localisation of a series of dipeptide-based vinyl sulfones.

Doherty W, James J, Evans P, Martin L, Adler N, Nolan D, Knox A.

Org Biomol Chem. 2014 Oct 14;12(38):7561-71. doi: 10.1039/c4ob01412j.

PMID:
25137249
4.

Aryl ureas represent a new class of anti-trypanosomal agents.

Du X, Hansell E, Engel JC, Caffrey CR, Cohen FE, McKerrow JH.

Chem Biol. 2000 Sep;7(9):733-42.

5.

Synthesis of macrocyclic trypanosomal cysteine protease inhibitors.

Chen YT, Lira R, Hansell E, McKerrow JH, Roush WR.

Bioorg Med Chem Lett. 2008 Nov 15;18(22):5860-3. doi: 10.1016/j.bmcl.2008.06.012. Epub 2008 Jun 10.

6.

The Inhibition of Cysteine Proteases Rhodesain and TbCatB: A Valuable Approach to Treat Human African Trypanosomiasis.

Ettari R, Previti S, Tamborini L, Cullia G, Grasso S, ZappalĂ  M.

Mini Rev Med Chem. 2016;16(17):1374-1391. Review.

PMID:
27156518
7.

Trypanocidal activities of trileucine methyl vinyl sulfone proteasome inhibitors.

Steverding D, Spackman RW, Royle HJ, Glenn RJ.

Parasitol Res. 2005 Jan;95(1):73-6. Epub 2004 Dec 1.

PMID:
15578221
8.

Design and synthesis of peptidomimetic protein farnesyltransferase inhibitors as anti-Trypanosoma brucei agents.

Ohkanda J, Buckner FS, Lockman JW, Yokoyama K, Carrico D, Eastman R, de Luca-Fradley K, Davies W, Croft SL, Van Voorhis WC, Gelb MH, Sebti SM, Hamilton AD.

J Med Chem. 2004 Jan 15;47(2):432-45.

PMID:
14711313
9.

Structure-guided development of selective TbcatB inhibitors.

Mallari JP, Shelat AA, Kosinski A, Caffrey CR, Connelly M, Zhu F, McKerrow JH, Guy RK.

J Med Chem. 2009 Oct 22;52(20):6489-93. doi: 10.1021/jm900908p.

10.

Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB.

Mallari JP, Shelat A, Kosinski A, Caffrey CR, Connelly M, Zhu F, McKerrow JH, Guy RK.

Bioorg Med Chem Lett. 2008 May 1;18(9):2883-5. doi: 10.1016/j.bmcl.2008.03.083. Epub 2008 Apr 8.

11.

Screening of acyl hydrazide proteinase inhibitors for antiparasitic activity against Trypanosoma brucei.

Caffrey CR, Schanz M, Nkemngu NJ, Brush M, Hansell E, Cohen FE, Flaherty TM, McKerrow JH, Steverding D.

Int J Antimicrob Agents. 2002 Mar;19(3):227-31. Erratum in: Int J Antimicrob Agents. 2005 Jul;26(1):100. Nkemgu-Njinkeng, Joseph [corrected to Nkemngu, Njinkeng Joseph]. Int J Antimicrob Agents. 2005 Nov;26(5):424.

PMID:
11932146
12.

Improved trypanocidal activities of cathepsin L inhibitors.

Nkemgu NJ, Grande R, Hansell E, McKerrow JH, Caffrey CR, Steverding D.

Int J Antimicrob Agents. 2003 Aug;22(2):155-9.

PMID:
12927956
13.

Trypanocidal activity of peptidyl vinyl ester derivatives selective for inhibition of mammalian proteasome trypsin-like activity.

Steverding D, Baldisserotto A, Wang X, Marastoni M.

Exp Parasitol. 2011 Aug;128(4):444-7. doi: 10.1016/j.exppara.2011.03.015. Epub 2011 Mar 31.

PMID:
21458452
14.

Crystal Structures of TbCatB and rhodesain, potential chemotherapeutic targets and major cysteine proteases of Trypanosoma brucei.

Kerr ID, Wu P, Marion-Tsukamaki R, Mackey ZB, Brinen LS.

PLoS Negl Trop Dis. 2010 Jun 8;4(6):e701. doi: 10.1371/journal.pntd.0000701.

15.

Development of potent purine-derived nitrile inhibitors of the trypanosomal protease TbcatB.

Mallari JP, Shelat AA, Obrien T, Caffrey CR, Kosinski A, Connelly M, Harbut M, Greenbaum D, McKerrow JH, Guy RK.

J Med Chem. 2008 Feb 14;51(3):545-52. doi: 10.1021/jm070760l. Epub 2008 Jan 4.

PMID:
18173229
16.

Development of novel 1,4-benzodiazepine-based Michael acceptors as antitrypanosomal agents.

Ettari R, Previti S, Cosconati S, Maiorana S, Schirmeister T, Grasso S, ZappalĂ  M.

Bioorg Med Chem Lett. 2016 Aug 1;26(15):3453-6. doi: 10.1016/j.bmcl.2016.06.047. Epub 2016 Jun 21.

PMID:
27372809
17.

Active site mapping, biochemical properties and subcellular localization of rhodesain, the major cysteine protease of Trypanosoma brucei rhodesiense.

Caffrey CR, Hansell E, Lucas KD, Brinen LS, Alvarez Hernandez A, Cheng J, Gwaltney SL 2nd, Roush WR, Stierhof YD, Bogyo M, Steverding D, McKerrow JH.

Mol Biochem Parasitol. 2001 Nov;118(1):61-73.

PMID:
11704274
18.

Design, synthesis, and evaluation of inhibitors of trypanosomal and leishmanial dihydrofolate reductase.

Chowdhury SF, Villamor VB, Guerrero RH, Leal I, Brun R, Croft SL, Goodman JM, Maes L, Ruiz-Perez LM, Pacanowska DG, Gilbert IH.

J Med Chem. 1999 Oct 21;42(21):4300-12.

PMID:
10543874
19.

In vitro effect of alkaloids on bloodstream forms of Trypanosoma brucei and T. congolense.

Merschjohann K, Sporer F, Steverding D, Wink M.

Planta Med. 2001 Oct;67(7):623-7.

PMID:
11582539
20.

Synthesis and structure-activity relationships of parasiticidal thiosemicarbazone cysteine protease inhibitors against Plasmodium falciparum, Trypanosoma brucei, and Trypanosoma cruzi.

Greenbaum DC, Mackey Z, Hansell E, Doyle P, Gut J, Caffrey CR, Lehrman J, Rosenthal PJ, McKerrow JH, Chibale K.

J Med Chem. 2004 Jun 3;47(12):3212-9.

PMID:
15163200

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