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Items: 1 to 20 of 115

1.

Assessing the trypanocidal potential of natural and semi-synthetic diketopiperazines from two deep water marine-derived fungi.

Watts KR, Ratnam J, Ang KH, Tenney K, Compton JE, McKerrow J, Crews P.

Bioorg Med Chem. 2010 Apr 1;18(7):2566-74. doi: 10.1016/j.bmc.2010.02.034. Epub 2010 Mar 1.

2.

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.

3.

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
4.

Evaluation of trypanocidal activity of combinations of anti-sleeping sickness drugs with cysteine protease inhibitors.

Steverding D.

Exp Parasitol. 2015 Apr-May;151-152:28-33. doi: 10.1016/j.exppara.2015.01.016. Epub 2015 Feb 4.

PMID:
25662707
5.

Chalcone, acyl hydrazide, and related amides kill cultured Trypanosoma brucei brucei.

Troeberg L, Chen X, Flaherty TM, Morty RE, Cheng M, Hua H, Springer C, McKerrow JH, Kenyon GL, Lonsdale-Eccles JD, Coetzer TH, Cohen FE.

Mol Med. 2000 Aug;6(8):660-9.

6.

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
7.

Hit-to-lead development of the chamigrane endoperoxide merulin A for the treatment of African sleeping sickness.

Navarro G, Chokpaiboon S, De Muylder G, Bray WM, Nisam SC, McKerrow JH, Pudhom K, Linington RG.

PLoS One. 2012;7(9):e46172. doi: 10.1371/journal.pone.0046172. Epub 2012 Sep 27.

8.

Inhibition of rhodesain as a novel therapeutic modality for human African trypanosomiasis.

Ettari R, Tamborini L, Angelo IC, Micale N, Pinto A, De Micheli C, Conti P.

J Med Chem. 2013 Jul 25;56(14):5637-58. doi: 10.1021/jm301424d. Epub 2013 May 7.

PMID:
23611656
9.

Novel lipophilic acetohydroxamic acid derivatives based on conformationally constrained spiro carbocyclic 2,6-diketopiperazine scaffolds with potent trypanocidal activity.

Fytas C, Zoidis G, Tzoutzas N, Taylor MC, Fytas G, Kelly JM.

J Med Chem. 2011 Jul 28;54(14):5250-4. doi: 10.1021/jm200217m. Epub 2011 Jun 27.

10.

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
11.

Antibacterial activity of diketopiperazines isolated from a marine fungus using t-butoxycarbonyl group as a simple tool for purification.

El-Gendy Bel-D, Rateb ME.

Bioorg Med Chem Lett. 2015 Aug 15;25(16):3125-8. doi: 10.1016/j.bmcl.2015.06.010. Epub 2015 Jun 9.

PMID:
26099531
12.

2,5-diketopiperazines from the marine-derived fungus Aspergillus fumigatus YK-7.

Wang Y, Li ZL, Bai J, Zhang LM, Wu X, Zhang L, Pei YH, Jing YK, Hua HM.

Chem Biodivers. 2012 Feb;9(2):385-93. doi: 10.1002/cbdv.201100061.

PMID:
22344914
13.

3-(Oxazolo[4,5-b]pyridin-2-yl)anilides as a novel class of potent inhibitors for the kinetoplastid Trypanosoma brucei, the causative agent for human African trypanosomiasis.

Ferrins L, Rahmani R, Sykes ML, Jones AJ, Avery VM, Teston E, Almohaywi B, Yin J, Smith J, Hyland C, White KL, Ryan E, Campbell M, Charman SA, Kaiser M, Baell JB.

Eur J Med Chem. 2013 Aug;66:450-65. doi: 10.1016/j.ejmech.2013.05.007. Epub 2013 May 16.

PMID:
23831695
14.

Identification of compounds with anti-proliferative activity against Trypanosoma brucei brucei strain 427 by a whole cell viability based HTS campaign.

Sykes ML, Baell JB, Kaiser M, Chatelain E, Moawad SR, Ganame D, Ioset JR, Avery VM.

PLoS Negl Trop Dis. 2012;6(11):e1896. doi: 10.1371/journal.pntd.0001896. Epub 2012 Nov 29.

15.

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.

16.

Antitrypanosomal structure-activity-relationship study of synthetic cynaropicrin derivatives.

Usuki T, Sato M, Hara S, Yoshimoto Y, Kondo R, Zimmermann S, Kaiser M, Brun R, Hamburger M, Adams M.

Bioorg Med Chem Lett. 2014 Feb 1;24(3):794-8. doi: 10.1016/j.bmcl.2013.12.099. Epub 2014 Jan 2.

PMID:
24433861
17.

Cysteine proteinase inhibitors kill cultured bloodstream forms of Trypanosoma brucei brucei.

Troeberg L, Morty RE, Pike RN, Lonsdale-Eccles JD, Palmer JT, McKerrow JH, Coetzer TH.

Exp Parasitol. 1999 Apr;91(4):349-55.

PMID:
10092479
18.

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
19.

Trypanocidal activity of marine natural products.

Jones AJ, Grkovic T, Sykes ML, Avery VM.

Mar Drugs. 2013 Oct 22;11(10):4058-82. doi: 10.3390/md11104058. Review.

20.

Non-natural acetogenin analogues as potent Trypanosoma brucei inhibitors.

Florence GJ, Fraser AL, Gould ER, King EF, Menzies SK, Morris JC, Tulloch LB, Smith TK.

ChemMedChem. 2014 Nov;9(11):2548-56. doi: 10.1002/cmdc.201402272. Epub 2014 Aug 21.

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