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Experimental Therapeutics

Identification of a New Amide-Containing Thiazole as a Drug Candidate for Treatment of Chagas' Disease

Guzmán Álvarez, Javier Varela, Eugenia Cruces, Marcelo Fernández, Martín Gabay, Sandra M. Leal, Patricia Escobar, Luis Sanabria, Elva Serna, Susana Torres, Susy J. Figueredo Thiel, Gloria Yaluff, Ninfa I. Vera de Bilbao, Hugo Cerecetto, Mercedes González
Guzmán Álvarez
aGrupo de Química Medicinal, Laboratorio de Química Orgánica, Facultad de Ciencias, Universidad de la República, Montevideo, Uruguay
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Javier Varela
aGrupo de Química Medicinal, Laboratorio de Química Orgánica, Facultad de Ciencias, Universidad de la República, Montevideo, Uruguay
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Eugenia Cruces
aGrupo de Química Medicinal, Laboratorio de Química Orgánica, Facultad de Ciencias, Universidad de la República, Montevideo, Uruguay
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Marcelo Fernández
bLaboratorio de Experimentación Animal, Centro de Investigaciones Nucleares, Facultad de Ciencias, Universidad de la República, Montevideo, Uruguay
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Martín Gabay
aGrupo de Química Medicinal, Laboratorio de Química Orgánica, Facultad de Ciencias, Universidad de la República, Montevideo, Uruguay
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Sandra M. Leal
cCentro de Investigaciones de Enfermedades Tropicales, Departamento de Ciencias Básicas, Universidad Industrial de Santander, Bucaramanga, Colombia
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Patricia Escobar
cCentro de Investigaciones de Enfermedades Tropicales, Departamento de Ciencias Básicas, Universidad Industrial de Santander, Bucaramanga, Colombia
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Luis Sanabria
dDepartamento de Medicina Tropical, Instituto de Investigaciones en Ciencias de la Salud, Universidad Nacional de Asunción, Asunción, Paraguay
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Elva Serna
dDepartamento de Medicina Tropical, Instituto de Investigaciones en Ciencias de la Salud, Universidad Nacional de Asunción, Asunción, Paraguay
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Susana Torres
dDepartamento de Medicina Tropical, Instituto de Investigaciones en Ciencias de la Salud, Universidad Nacional de Asunción, Asunción, Paraguay
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Susy J. Figueredo Thiel
eDepartamento de Anatomía Patológica, Instituto de Investigaciones en Ciencias de la Salud, Universidad Nacional de Asunción, Asunción, Paraguay
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Gloria Yaluff
dDepartamento de Medicina Tropical, Instituto de Investigaciones en Ciencias de la Salud, Universidad Nacional de Asunción, Asunción, Paraguay
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Ninfa I. Vera de Bilbao
dDepartamento de Medicina Tropical, Instituto de Investigaciones en Ciencias de la Salud, Universidad Nacional de Asunción, Asunción, Paraguay
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Hugo Cerecetto
aGrupo de Química Medicinal, Laboratorio de Química Orgánica, Facultad de Ciencias, Universidad de la República, Montevideo, Uruguay
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Mercedes González
aGrupo de Química Medicinal, Laboratorio de Química Orgánica, Facultad de Ciencias, Universidad de la República, Montevideo, Uruguay
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DOI: 10.1128/AAC.03814-14
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ABSTRACT

Although the parasitic infection Chagas' disease was described over 100 years ago, even now there are not suitable drugs. The available drugs nifurtimox and benznidazole have limited efficacies and tolerances, with proven mutagenic effects. Attempting to find appropriate drugs to deal with this problem, here we report on the development and pharmacological characterization of new amide-containing thiazoles. In the present study, we evaluated the in vitro and in vivo effects of new candidates against Trypanosoma cruzi, the etiological agent of Chagas' disease. The lead amide-containing thiazole derivative had potent in vitro activity, an absence of both in vitro mutagenic and in vivo clastogenic effects, and excellent in vitro selectivity and in vivo tolerance. The compound suppressed parasitemia in mice, modifying the anti-T. cruzi antibodies like the reference drug, benznidazole, and displayed the lowest mortality among the tested drugs. The present evidence suggests that this compound is a promising anti-T. cruzi agent surpassing the lead optimization stage in drug development and leading to a candidate for preclinical study.

FOOTNOTES

    • Received 6 July 2014.
    • Returned for modification 5 August 2014.
    • Accepted 28 November 2014.
    • Accepted manuscript posted online 15 December 2014.
  • Supplemental material for this article may be found at http://dx.doi.org/10.1128/AAC.03814-14.

  • Copyright © 2015, American Society for Microbiology. All Rights Reserved.
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Identification of a New Amide-Containing Thiazole as a Drug Candidate for Treatment of Chagas' Disease
Guzmán Álvarez, Javier Varela, Eugenia Cruces, Marcelo Fernández, Martín Gabay, Sandra M. Leal, Patricia Escobar, Luis Sanabria, Elva Serna, Susana Torres, Susy J. Figueredo Thiel, Gloria Yaluff, Ninfa I. Vera de Bilbao, Hugo Cerecetto, Mercedes González
Antimicrobial Agents and Chemotherapy Feb 2015, 59 (3) 1398-1404; DOI: 10.1128/AAC.03814-14

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Identification of a New Amide-Containing Thiazole as a Drug Candidate for Treatment of Chagas' Disease
Guzmán Álvarez, Javier Varela, Eugenia Cruces, Marcelo Fernández, Martín Gabay, Sandra M. Leal, Patricia Escobar, Luis Sanabria, Elva Serna, Susana Torres, Susy J. Figueredo Thiel, Gloria Yaluff, Ninfa I. Vera de Bilbao, Hugo Cerecetto, Mercedes González
Antimicrobial Agents and Chemotherapy Feb 2015, 59 (3) 1398-1404; DOI: 10.1128/AAC.03814-14
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