Synthesis and antiparasitic activity of 2-(trifluoromethyl)-benzimidazole derivatives

2-(Trifluoromethyl)benzimidazole derivatives substituted at the 1-, 5-, and 6-positions have been synthesized and in vitro tested against the protozoa Giardia lamblia, Entamnoeha histolytica. and the helminth Trichinella spiralis. Results indicate that all the compounds tested are more active as ant...

Full description

Saved in:
Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2001-01, Vol.11 (2), p.187-190
Main Authors: NAVARRETE-VAZQUEZ, Gabriel, CEDILLO, Roberto, HERNANDEZ-CAMPOS, Alicia, YEPEZ, Lilian, HERNANDEZ-LUIS, Francisco, VALDEZ, Juan, MORALES, Raul, CORTES, Rafael, HERNANDEZ, Manuel, CASTILLO, Rafael
Format: Article
Language:English
Subjects:
Animals
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiparasitic agents
Antiparasitic Agents - chemical synthesis
Benzimidazoles - chemical synthesis
Benzimidazoles - chemistry
Benzimidazoles - pharmacology
Biological and medical sciences
Brain Chemistry - drug effects
Entamoeba histolytica - drug effects
Fluorine Compounds - chemistry
Giardia lamblia - drug effects
Larva - drug effects
Medical sciences
Pharmacology. Drug treatments
Rats
Rats, Wistar
Trichinella spiralis - drug effects
Tubulin - drug effects
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:2-(Trifluoromethyl)benzimidazole derivatives substituted at the 1-, 5-, and 6-positions have been synthesized and in vitro tested against the protozoa Giardia lamblia, Entamnoeha histolytica. and the helminth Trichinella spiralis. Results indicate that all the compounds tested are more active as antiprotozoal agents than Albendazole and Metronidazole. One compound (20) was as active as Albendazole against T. spiralis. These compounds were also tested for their effect on tubulin polymerization and none inhibited tubulin polymerization.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(00)00619-3