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Items: 1 to 20 of 137

1.

Discovery of N-(4-sulfamoylphenyl)thioureas as Trypanosoma brucei leucyl-tRNA synthetase inhibitors.

Zhang F, Du J, Wang Q, Hu Q, Zhang J, Ding D, Zhao Y, Yang F, Wang E, Zhou H.

Org Biomol Chem. 2013 Aug 28;11(32):5310-24. doi: 10.1039/c3ob40236c.

PMID:
23842857
2.

Identification of Trypanosoma brucei leucyl-tRNA synthetase inhibitors by pharmacophore- and docking-based virtual screening and synthesis.

Zhao Y, Wang Q, Meng Q, Ding D, Yang H, Gao G, Li D, Zhu W, Zhou H.

Bioorg Med Chem. 2012 Feb 1;20(3):1240-50. doi: 10.1016/j.bmc.2011.12.035. Epub 2011 Dec 30.

PMID:
22249121
3.

Design, synthesis, and structure-activity relationship of Trypanosoma brucei leucyl-tRNA synthetase inhibitors as antitrypanosomal agents.

Ding D, Meng Q, Gao G, Zhao Y, Wang Q, Nare B, Jacobs R, Rock F, Alley MR, Plattner JJ, Chen G, Li D, Zhou H.

J Med Chem. 2011 Mar 10;54(5):1276-87. doi: 10.1021/jm101225g. Epub 2011 Feb 15.

PMID:
21322634
4.

Computer-aided discovery of Trypanosoma brucei RNA-editing terminal uridylyl transferase 2 inhibitors.

Demir O, Labaied M, Merritt C, Stuart K, Amaro RE.

Chem Biol Drug Des. 2014 Aug;84(2):131-9. doi: 10.1111/cbdd.12302. Epub 2014 Jun 5.

5.

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
6.

Parasite-based screening and proteome profiling reveal orlistat, an FDA-approved drug, as a potential anti Trypanosoma brucei agent.

Yang PY, Wang M, Liu K, Ngai MH, Sheriff O, Lear MJ, Sze SK, He CY, Yao SQ.

Chemistry. 2012 Jul 2;18(27):8403-13. doi: 10.1002/chem.201200482. Epub 2012 Jun 1.

PMID:
22674877
7.

Inhibition of isoleucyl-tRNA synthetase as a potential treatment for human African Trypanosomiasis.

Cestari I, Stuart K.

J Biol Chem. 2013 May 17;288(20):14256-63. doi: 10.1074/jbc.M112.447441. Epub 2013 Apr 2.

8.

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.

9.

Induced resistance to methionyl-tRNA synthetase inhibitors in Trypanosoma brucei is due to overexpression of the target.

Ranade RM, Gillespie JR, Shibata S, Verlinde CL, Fan E, Hol WG, Buckner FS.

Antimicrob Agents Chemother. 2013 Jul;57(7):3021-8. doi: 10.1128/AAC.02578-12. Epub 2013 Apr 15.

10.

Design and Synthesis of Brain Penetrant Trypanocidal N-Myristoyltransferase Inhibitors.

Bayliss T, Robinson DA, Smith VC, Brand S, McElroy SP, Torrie LS, Mpamhanga C, Norval S, Stojanovski L, Brenk R, Frearson JA, Read KD, Gilbert IH, Wyatt PG.

J Med Chem. 2017 Dec 14;60(23):9790-9806. doi: 10.1021/acs.jmedchem.7b01255. Epub 2017 Nov 22.

11.

Design, synthesis and biological evaluation of Trypanosoma brucei trypanothione synthetase inhibitors.

Spinks D, Torrie LS, Thompson S, Harrison JR, Frearson JA, Read KD, Fairlamb AH, Wyatt PG, Gilbert IH.

ChemMedChem. 2012 Jan 2;7(1):95-106. doi: 10.1002/cmdc.201100420. Epub 2011 Dec 8.

12.

Discovery of Indoline-2-carboxamide Derivatives as a New Class of Brain-Penetrant Inhibitors of Trypanosoma brucei.

Cleghorn LA, Albrecht S, Stojanovski L, Simeons FR, Norval S, Kime R, Collie IT, De Rycker M, Campbell L, Hallyburton I, Frearson JA, Wyatt PG, Read KD, Gilbert IH.

J Med Chem. 2015 Oct 8;58(19):7695-706. doi: 10.1021/acs.jmedchem.5b00596. Epub 2015 Sep 29.

13.

5-Fluoroimidazo[4,5-b]pyridine Is a Privileged Fragment That Conveys Bioavailability to Potent Trypanosomal Methionyl-tRNA Synthetase Inhibitors.

Zhang Z, Koh CY, Ranade RM, Shibata S, Gillespie JR, Hulverson MA, Huang W, Nguyen J, Pendem N, Gelb MH, Verlinde CL, Hol WG, Buckner FS, Fan E.

ACS Infect Dis. 2016 Jun 10;2(6):399-404. doi: 10.1021/acsinfecdis.6b00036. Epub 2016 Apr 11.

14.

Investigation of trypanothione reductase as a drug target in Trypanosoma brucei.

Spinks D, Shanks EJ, Cleghorn LA, McElroy S, Jones D, James D, Fairlamb AH, Frearson JA, Wyatt PG, Gilbert IH.

ChemMedChem. 2009 Dec;4(12):2060-9. doi: 10.1002/cmdc.200900262.

15.

Cruzain inhibitors: efforts made, current leads and a structural outlook of new hits.

Martinez-Mayorga K, Byler KG, Ramirez-Hernandez AI, Terrazas-Alvares DE.

Drug Discov Today. 2015 Jul;20(7):890-8. doi: 10.1016/j.drudis.2015.02.004. Epub 2015 Feb 16. Review.

PMID:
25697479
16.

Synthesis and assessment of catechol diether compounds as inhibitors of trypanosomal phosphodiesterase B1 (TbrPDEB1).

Woodring JL, Bland ND, Ochiana SO, Campbell RK, Pollastri MP.

Bioorg Med Chem Lett. 2013 Nov 1;23(21):5971-4. doi: 10.1016/j.bmcl.2013.08.057. Epub 2013 Aug 21.

17.

Novel pyrrolobenzoxaboroles: design, synthesis, and biological evaluation against Trypanosoma brucei.

Wu P, Zhang J, Meng Q, Nare B, Jacobs RT, Zhou H.

Eur J Med Chem. 2014 Jun 23;81:59-75. doi: 10.1016/j.ejmech.2014.04.079. Epub 2014 Apr 29.

PMID:
24826816
18.

Discovery and antiparasitic activity of AZ960 as a Trypanosoma brucei ERK8 inhibitor.

Valenciano AL, Ramsey AC, Santos WL, Mackey ZB.

Bioorg Med Chem. 2016 Oct 1;24(19):4647-4651. doi: 10.1016/j.bmc.2016.07.069. Epub 2016 Aug 1.

PMID:
27519462
19.

Discovery of halo-nitrobenzamides with potential application against human African trypanosomiasis.

Hwang JY, Smithson D, Connelly M, Maier J, Zhu F, Guy KR.

Bioorg Med Chem Lett. 2010 Jan 1;20(1):149-52. doi: 10.1016/j.bmcl.2009.11.022. Epub 2009 Nov 14.

PMID:
19963377
20.

Identification of novel inhibitors of UDP-Glc 4'-epimerase, a validated drug target for african sleeping sickness.

Urbaniak MD, Tabudravu JN, Msaki A, Matera KM, Brenk R, Jaspars M, Ferguson MA.

Bioorg Med Chem Lett. 2006 Nov 15;16(22):5744-7. Epub 2006 Sep 7.

PMID:
16962325

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