2-alkylaminoethyl-1,1-bisphosphonic acids are potent inhibitors of the enzymatic activity of Trypanosoma cruzi squalene synthase

As part of our efforts aimed at searching for new antiparasitic agents, the effect of representative 2-alkylaminoethyl-1,1-bisphosphonic acids on Trypanosoma cruzi squalene synthase (TcSQS) was investigated. These compounds had proven to be potent inhibitors of T. cruzi. This cellular activity had b...

Descripción completa

Guardado en:
Detalles Bibliográficos
Autores principales: Szajnman, Sergio Hernán, Rodríguez, Juan Bautista
Publicado: 2012
Materias:
1,1 bisphosphonic acid derivative
bisphosphonic acid derivative
geranyltransferase
squalene synthase
squalene synthase inhibitor
unclassified drug
article
drug effect
drug mechanism
drug potency
enzyme activity
enzyme inhibition
IC 50
nonhuman
priority journal
Trypanosoma cruzi
Antiparasitic Agents
Chagas Disease
Diphosphonates
Farnesyl-Diphosphate Farnesyltransferase
Geranyltranstransferase
Parasitic Sensitivity Tests
Structure-Activity Relationship
Trypanocidal Agents
Acceso en línea:https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00664804_v56_n8_p4483_RodriguesPoveda
http://hdl.handle.net/20.500.12110/paper_00664804_v56_n8_p4483_RodriguesPoveda
Aporte de:
Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) de Universidad de Buenos Aires
Descripción
Sumario:As part of our efforts aimed at searching for new antiparasitic agents, the effect of representative 2-alkylaminoethyl-1,1-bisphosphonic acids on Trypanosoma cruzi squalene synthase (TcSQS) was investigated. These compounds had proven to be potent inhibitors of T. cruzi. This cellular activity had been associated with an inhibition of the enzymatic activity of T. cruzi farnesyl diphosphate synthase. 2-Alkylaminoethyl-1,1-bisphosphonic acids appear to have a dual action, since they also inhibit TcSQS at the nanomolar range. Copyright © 2012, American Society for Microbiology. All Rights Reserved.

Ejemplares similares