title: Synthesis and trypanocidal activity of novel benzimidazole derivatives.
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).
authors: Facultad de Química, Departamento de Farmacia, Universidad Nacional Autónoma de México, México, DF 04510, Mexico.
authors: José Miguel
authors: JM
authors: Velázquez-López
authors: Facultad de Química, Departamento de Farmacia, Universidad Nacional Autónoma de México, México, DF 04510, Mexico.
authors: Alicia
authors: A
authors: Hernández-Campos
authors: Unidad de Investigación Médica en Enfermedades Infecciosas y Parasitarias, IMSS, México, DF 06720, Mexico.
authors: Lilián
authors: L
authors: Yépez-Mulia
authors: Facultad de Medicina y Nutrición, Centro de Investigación en Alimentos y Nutrición, Universidad Juárez del Estado de Durango, Durango 34000, Mexico.
authors: Alfredo
authors: A
authors: Téllez-Valencia
authors: Facultad de Química, Departamento de Farmacia, Universidad Nacional Autónoma de México, México, DF 04510, Mexico.
authors: Paulina
authors: P
authors: Flores-Carrillo
authors: Escuela Nacional de Ciencias Biológicas, Departamento de Parasitología, IPN, México, DF 11340, Mexico.
authors: Rocío
authors: R
authors: Nieto-Meneses
authors: Facultad de Química, Departamento de Farmacia, Universidad Nacional Autónoma de México, México, DF 04510, Mexico. Electronic address: rafaelc@unam.mx.
authors: Rafael
authors: R
authors: Castillo
mesh_terms: D000818:Animals; D000977:Antiparasitic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D051379:Mice; D015394:Molecular Structure; D014349:Trypanosoma cruzi / Q000187:drug effects*
chemical_list: D000977:Antiparasitic Agents; D001562:Benzimidazoles
keywords: Benzimidazole derivatives; Chagas disease; Triosephosphate isomerase; Trypanosoma cruzi