RT info:eu-repo/semantics/article
T1 Benzimidazole and aminoalcohol derivatives show in vitro anthelmintic activity against Trichuris muris and Heligmosomoides polygyrus
A1 Valderas García, Elora
A1 Häberli, Cécile
A1 Álvarez Bardón, María
A1 Escala, Nerea
A1 Castilla Gómez de Agüero, Verónica
A1 Vega, Jennifer de la
A1 Olmo, Esther del
A1 Balaña Fouce, Rafael
A1 Keiser, Jennifer
A1 Martínez Valladares, María
A2 Sanidad Animal
K1 Sanidad animal
K1 Veterinaria
K1 Trichuris muris
K1 Heligmosomoides polygyrus
K1 Anthelmintic
K1 Benzimidazol
K1 Diamine
K1 Aminoalcohol
K1 3109 Ciencias Veterinarias
K1 2401.12 Parasitología Animal
K1 3207.12 Parasitología
AB [EN]Background: Infections by gastrointestinal nematodes cause significant economic losses and disease in both humans and animals worldwide. The discovery of novel anthelmintic drugs is crucial for maintaining control of these parasitic infections. Methods: For this purpose, the aim of the present study was to evaluate the potential anthelmintic activity of three series of compounds against the gastrointestinal nematodes Trichuris muris and Heligmosomoides polygyrus in vitro. The compounds tested were derivatives of benzimidazole, lipidic aminoalcohols and diamines. A primary screening was performed to select those compounds with an ability to inhibit T. muris L1 motility by > 90% at a single concentration of 100 µM; then, their respective IC50 values were calculated. Those compounds with IC50 < 10 µM were also tested against the adult stage of T. muris and H. polygyrus at a single concentration of 10 µM. Results: Of the 41 initial compounds screened, only compounds AO14, BZ6 and BZ12 had IC50 values < 10 µM on T. muris L1 assay, showing IC50 values of 3.30, 8.89 and 4.17 µM, respectively. However, only two of them displayed activity against the adult stage of the parasites: BZ12 killed 81% of adults of T. muris (IC50 of 8.1 µM) and 53% of H. polygyrus while BZ6 killed 100% of H. polygyrus adults (IC50 of 5.3 µM) but only 17% of T. muris. Conclusions: BZ6 and BZ12 could be considered as a starting point for the synthesis of further structurally related compounds.
PB BMC
LK https://hdl.handle.net/10612/18709
UL https://hdl.handle.net/10612/18709
NO Valderas-García, E., Häberli, C., Álvarez-Bardón, M., Escala, N., Castilla-Gómez de Agüero, V., de la Vega, J., del Olmo, E., Balaña-Fouce, R., Keiser, J., & Martínez-Valladares, M. (2022). Benzimidazole and aminoalcohol derivatives show in vitro anthelmintic activity against Trichuris muris and Heligmosomoides polygyrus. Parasites and Vectors, 15(1). https://doi.org/10.1186/S13071-022-05347-Y
DS BULERIA. Repositorio Institucional de la Universidad de León
RD 14-jun-2024