2. Academic Validation
  3. Synthesis and trypanocidal activity of novel benzimidazole derivatives

Synthesis and trypanocidal activity of novel benzimidazole derivatives

  • Bioorg Med Chem Lett. 2016 Sep 1;26(17):4377-81. doi: 10.1016/j.bmcl.2015.08.018.
José Miguel Velázquez-López 1,  Alicia Hernández-Campos 1,  Lilián Yépez-Mulia 2,  Alfredo Téllez-Valencia 3,  Paulina Flores-Carrillo 1,  Rocío Nieto-Meneses 4,  Rafael Castillo 5
Affiliations

Affiliations

  • 1 Facultad de Química, Departamento de Farmacia, Universidad Nacional Autónoma de México, México, DF 04510, Mexico.
  • 2 Unidad de Investigación Médica en Enfermedades Infecciosas y Parasitarias, IMSS, México, DF 06720, Mexico.
  • 3 Facultad de Medicina y Nutrición, Centro de Investigación en Alimentos y Nutrición, Universidad Juárez del Estado de Durango, Durango 34000, Mexico.
  • 4 Escuela Nacional de Ciencias Biológicas, Departamento de Parasitología, IPN, México, DF 11340, Mexico.
  • 5 Facultad de Química, Departamento de Farmacia, Universidad Nacional Autónoma de México, México, DF 04510, Mexico. Electronic address: rafaelc@unam.mx.
PMID: 27503677 DOI: 10.1016/j.bmcl.2015.08.018
Abstract

The present work reports the synthesis and biological activity of a series of 14 benzimidazole derivatives designed to act on the Enzyme triosephosphate isomerase of Trypanosoma cruzi (TcTIM). This Enzyme is involved in the metabolism of glucose, the only source of energy for the Parasite. In this study, we found four compounds that inhibit TcTIM moderately and lack inhibitory activity against human TIM (HsTIM). In vitro studies against T. cruzi epimastigotes showed two compounds that were more active than the reference drug nifurtimox, and these presented a low cytotoxic effect in mouse macrophages (J744 cell line).

Keywords

Benzimidazole derivatives; Chagas disease; Triosephosphate isomerase; Trypanosoma cruzi.

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