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Development of novel drugs for human African trypanosomiasis.

Brun R, Don R, Jacobs RT, Wang MZ, Barrett MP.

Future Microbiol. 2011 Jun;6(6):677-91. doi: 10.2217/fmb.11.44. Review.


Fexinidazole--a new oral nitroimidazole drug candidate entering clinical development for the treatment of sleeping sickness.

Torreele E, Bourdin Trunz B, Tweats D, Kaiser M, Brun R, Mazué G, Bray MA, Pécoul B.

PLoS Negl Trop Dis. 2010 Dec 21;4(12):e923. doi: 10.1371/journal.pntd.0000923.


Antitrypanosomal activity of fexinidazole, a new oral nitroimidazole drug candidate for treatment of sleeping sickness.

Kaiser M, Bray MA, Cal M, Bourdin Trunz B, Torreele E, Brun R.

Antimicrob Agents Chemother. 2011 Dec;55(12):5602-8. doi: 10.1128/AAC.00246-11. Epub 2011 Sep 12.


Benzoxaboroles: a new class of potential drugs for human African trypanosomiasis.

Jacobs RT, Plattner JJ, Nare B, Wring SA, Chen D, Freund Y, Gaukel EG, Orr MD, Perales JB, Jenks M, Noe RA, Sligar JM, Zhang YK, Bacchi CJ, Yarlett N, Don R.

Future Med Chem. 2011 Aug;3(10):1259-78. doi: 10.4155/fmc.11.80.


Do we need new drugs against human African trypanosomiasis?

Stich A, Ponte-Sucre A, Holzgrabe U.

Lancet Infect Dis. 2013 Sep;13(9):733-4. doi: 10.1016/S1473-3099(13)70191-9. No abstract available.


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.


Chemotherapy of second stage human African trypanosomiasis: comparison between the parenteral diamidine DB829 and its oral prodrug DB868 in vervet monkeys.

Thuita JK, Wolf KK, Murilla GA, Bridges AS, Boykin DW, Mutuku JN, Liu Q, Jones SK, Gem CO, Ching S, Tidwell RR, Wang MZ, Paine MF, Brun R.

PLoS Negl Trop Dis. 2015 Feb 5;9(2):e0003409. doi: 10.1371/journal.pntd.0003409. eCollection 2015 Feb.


Melarsoprol cyclodextrin inclusion complexes as promising oral candidates for the treatment of human African trypanosomiasis.

Rodgers J, Jones A, Gibaud S, Bradley B, McCabe C, Barrett MP, Gettinby G, Kennedy PG.

PLoS Negl Trop Dis. 2011 Sep;5(9):e1308. doi: 10.1371/journal.pntd.0001308. Epub 2011 Sep 6.


Potential new drugs for human African trypanosomiasis: some progress at last.

Barrett MP.

Curr Opin Infect Dis. 2010 Dec;23(6):603-8. doi: 10.1097/QCO.0b013e32833f9fd0. Review.


SCYX-7158, an orally-active benzoxaborole for the treatment of stage 2 human African trypanosomiasis.

Jacobs RT, Nare B, Wring SA, Orr MD, Chen D, Sligar JM, Jenks MX, Noe RA, Bowling TS, Mercer LT, Rewerts C, Gaukel E, Owens J, Parham R, Randolph R, Beaudet B, Bacchi CJ, Yarlett N, Plattner JJ, Freund Y, Ding C, Akama T, Zhang YK, Brun R, Kaiser M, Scandale I, Don R.

PLoS Negl Trop Dis. 2011 Jun;5(6):e1151. doi: 10.1371/journal.pntd.0001151. Epub 2011 Jun 28.


Genotoxicity profile of fexinidazole--a drug candidate in clinical development for human African trypanomiasis (sleeping sickness).

Tweats D, Bourdin Trunz B, Torreele E.

Mutagenesis. 2012 Sep;27(5):523-32. doi: 10.1093/mutage/ges015. Epub 2012 Apr 26.


Fexinidazole: a potential new drug candidate for Chagas disease.

Bahia MT, de Andrade IM, Martins TA, do Nascimento ÁF, Diniz Lde F, Caldas IS, Talvani A, Trunz BB, Torreele E, Ribeiro I.

PLoS Negl Trop Dis. 2012;6(11):e1870. doi: 10.1371/journal.pntd.0001870. Epub 2012 Nov 1.


In vivo imaging of trypanosome-brain interactions and development of a rapid screening test for drugs against CNS stage trypanosomiasis.

Myburgh E, Coles JA, Ritchie R, Kennedy PG, McLatchie AP, Rodgers J, Taylor MC, Barrett MP, Brewer JM, Mottram JC.

PLoS Negl Trop Dis. 2013 Aug 22;7(8):e2384. doi: 10.1371/journal.pntd.0002384. eCollection 2013.


Screening strategies to identify new chemical diversity for drug development to treat kinetoplastid infections.

Don R, Ioset JR.

Parasitology. 2014 Jan;141(1):140-6. doi: 10.1017/S003118201300142X. Epub 2013 Aug 28. Review. Erratum in: Parasitology. 2014 Jan;141(1):147.


Treatment of African trypanosomiasis with cordycepin and adenosine deaminase inhibitors in a mouse model.

Rottenberg ME, Masocha W, Ferella M, Petitto-Assis F, Goto H, Kristensson K, McCaffrey R, Wigzell H.

J Infect Dis. 2005 Nov 1;192(9):1658-65. Epub 2005 Sep 30.


Control and surveillance of human African trypanosomiasis.

World Health Organization.

World Health Organ Tech Rep Ser. 2013;(984):1-237.


The kinetoplastid chemotherapy revisited: current drugs, recent advances and future perspectives.

Castillo E, Dea-Ayuela MA, Bolás-Fernández F, Rangel M, González-Rosende ME.

Curr Med Chem. 2010;17(33):4027-51. Review.


Safety, pharmacokinetic, and efficacy studies of oral DB868 in a first stage vervet monkey model of human African trypanosomiasis.

Thuita JK, Wolf KK, Murilla GA, Liu Q, Mutuku JN, Chen Y, Bridges AS, Mdachi RE, Ismail MA, Ching S, Boykin DW, Hall JE, Tidwell RR, Paine MF, Brun R, Wang MZ.

PLoS Negl Trop Dis. 2013 Jun 6;7(6):e2230. doi: 10.1371/journal.pntd.0002230. Print 2013.


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.

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