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Design, structure-activity relationship and in vivo efficacy of piperazine analogues of fenarimol as inhibitors of Trypanosoma cruzi.

Keenan M, Alexander PW, Diao H, Best WM, Khong A, Kerfoot M, Thompson RC, White KL, Shackleford DM, Ryan E, Gregg AD, Charman SA, von Geldern TW, Scandale I, Chatelain E.

Bioorg Med Chem. 2013 Apr 1;21(7):1756-63. doi: 10.1016/j.bmc.2013.01.050. Epub 2013 Jan 31.


Analogues of fenarimol are potent inhibitors of Trypanosoma cruzi and are efficacious in a murine model of Chagas disease.

Keenan M, Abbott MJ, Alexander PW, Armstrong T, Best WM, Berven B, Botero A, Chaplin JH, Charman SA, Chatelain E, von Geldern TW, Kerfoot M, Khong A, Nguyen T, McManus JD, Morizzi J, Ryan E, Scandale I, Thompson RA, Wang SZ, White KL.

J Med Chem. 2012 May 10;55(9):4189-204. doi: 10.1021/jm2015809. Epub 2012 Apr 27.


Two analogues of fenarimol show curative activity in an experimental model of Chagas disease.

Keenan M, Chaplin JH, Alexander PW, Abbott MJ, Best WM, Khong A, Botero A, Perez C, Cornwall S, Thompson RA, White KL, Shackleford DM, Koltun M, Chiu FC, Morizzi J, Ryan E, Campbell M, von Geldern TW, Scandale I, Chatelain E, Charman SA.

J Med Chem. 2013 Dec 27;56(24):10158-70. doi: 10.1021/jm401610c. Epub 2013 Dec 4.


Conformational restriction of aryl thiosemicarbazones produces potent and selective anti-Trypanosoma cruzi compounds which induce apoptotic parasite death.

Magalhaes Moreira DR, de Oliveira AD, Teixeira de Moraes Gomes PA, de Simone CA, Villela FS, Ferreira RS, da Silva AC, dos Santos TA, Brelaz de Castro MC, Pereira VR, Leite AC.

Eur J Med Chem. 2014 Mar 21;75:467-78. doi: 10.1016/j.ejmech.2014.02.001. Epub 2014 Feb 3.


Pharmacological characterization, structural studies, and in vivo activities of anti-Chagas disease lead compounds derived from tipifarnib.

Buckner FS, Bahia MT, Suryadevara PK, White KL, Shackleford DM, Chennamaneni NK, Hulverson MA, Laydbak JU, Chatelain E, Scandale I, Verlinde CL, Charman SA, Lepesheva GI, Gelb MH.

Antimicrob Agents Chemother. 2012 Sep;56(9):4914-21. doi: 10.1128/AAC.06244-11. Epub 2012 Jul 9.


Trypanocidal activity of the phenyl-substituted analogue of furamidine DB569 against Trypanosoma cruzi infection in vivo.

de Souza EM, Oliveira GM, Boykin DW, Kumar A, Hu Q, De Nazaré C Soeiro M.

J Antimicrob Chemother. 2006 Sep;58(3):610-4. Epub 2006 Jul 19.


Selection and optimization of hits from a high-throughput phenotypic screen against Trypanosoma cruzi.

Keenan M, Alexander PW, Chaplin JH, Abbott MJ, Diao H, Wang Z, Best WM, Perez CJ, Cornwall SM, Keatley SK, Thompson RC, Charman SA, White KL, Ryan E, Chen G, Ioset JR, von Geldern TW, Chatelain E.

Future Med Chem. 2013 Oct;5(15):1733-52. doi: 10.4155/fmc.13.139.


Effects of juvenile hormone analogues (JHA) on the development of Trypanosoma cruzi.

Fichera L, Esteva M, Wimmer Z, Rodriguez JB, Gros EG.

Z Naturforsch C. 1995 Jul-Aug;50(7-8):578-80.


In vitro and in vivo studies of the trypanocidal activity of a diarylthiophene diamidine against Trypanosoma cruzi.

da Silva CF, Batista MM, Batista Dda G, de Souza EM, da Silva PB, de Oliveira GM, Meuser AS, Shareef AR, Boykin DW, Soeiro Mde N.

Antimicrob Agents Chemother. 2008 Sep;52(9):3307-14. doi: 10.1128/AAC.00038-08. Epub 2008 Jul 14.


Design, synthesis and cruzain docking of 3-(4-substituted-aryl)-1,2,4-oxadiazole-N-acylhydrazones as anti-Trypanosoma cruzi agents.

dos Santos Filho JM, Leite AC, de Oliveira BG, Moreira DR, Lima MS, Soares MB, Leite LF.

Bioorg Med Chem. 2009 Sep 15;17(18):6682-91. doi: 10.1016/j.bmc.2009.07.068. Epub 2009 Aug 6.


The urgent need to develop new drugs and tools for the treatment of Chagas disease.

Muñoz MJ, Murcia L, Segovia M.

Expert Rev Anti Infect Ther. 2011 Jan;9(1):5-7. doi: 10.1586/eri.10.144. No abstract available.


5-Nitro-2-furyl derivative actives against Trypanosoma cruzi: preliminary in vivo studies.

Cabrera E, Murguiondo MG, Arias MG, Arredondo C, Pintos C, Aguirre G, Fernández M, Basmadjián Y, Rosa R, Pacheco JP, Raymondo S, Di Maio R, González M, Cerecetto H.

Eur J Med Chem. 2009 Oct;44(10):3909-14. doi: 10.1016/j.ejmech.2009.04.015. Epub 2009 Apr 14.


Approaches for the development of new anti-Trypanosoma cruzi agents.

Moreira DR, Leite AC, dos Santos RR, Soares MB.

Curr Drug Targets. 2009 Mar;10(3):212-31. Review.


In vitro and in vivo trypanocidal activity of the ethyl esters of N-allyl and N-propyl oxamates using different Trypanosoma cruzi strains.

Aguirre-Alvarado C, Zaragoza-Martínez F, Rodríguez-Páez L, Nogueda B, Baeza I, Wong C.

J Enzyme Inhib Med Chem. 2007 Apr;22(2):227-33.


In vitro and in vivo trypanocidal effects of the cyclopalladated compound 7a, a drug candidate for treatment of Chagas' disease.

Matsuo AL, Silva LS, Torrecilhas AC, Pascoalino BS, Ramos TC, Rodrigues EG, Schenkman S, Caires AC, Travassos LR.

Antimicrob Agents Chemother. 2010 Aug;54(8):3318-25. doi: 10.1128/AAC.00323-10. Epub 2010 May 17.


Novel ruthenium complexes as potential drugs for Chagas's disease: enzyme inhibition and in vitro/in vivo trypanocidal activity.

Silva JJ, Guedes PM, Zottis A, Balliano TL, Nascimento Silva FO, França Lopes LG, Ellena J, Oliva G, Andricopulo AD, Franco DW, Silva JS.

Br J Pharmacol. 2010 May;160(2):260-9. doi: 10.1111/j.1476-5381.2009.00524.x. Epub 2010 Jan 26.


Experimental chemotherapy against Trypanosoma cruzi infection using ruthenium nitric oxide donors.

Silva JJ, Pavanelli WR, Pereira JC, Silva JS, Franco DW.

Antimicrob Agents Chemother. 2009 Oct;53(10):4414-21. doi: 10.1128/AAC.00104-09. Epub 2009 Jul 6.


Trypanothione reductase inhibition/trypanocidal activity relationships in a 1,4-bis(3-aminopropyl)piperazine series.

Bonnet B, Soullez D, Girault S, Maes L, Landry V, Davioud-Charvet E, Sergheraert C.

Bioorg Med Chem. 2000 Jan;8(1):95-103.


[The chemotherapy of Chagas disease].

Stoppani AO.

Medicina (B Aires). 1999;59 Suppl 2:147-65. Review. Spanish.


In vitro and in vivo activity of the chloroaryl-substituted imidazole viniconazole against Trypanosoma cruzi.

Silva CF, Batista Dda G, Batista MM, Lionel J, Hammer ER, Brun R, Soeiro Mde N.

Parasitology. 2014 Mar;141(3):367-73. doi: 10.1017/S0031182013001601.

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