The effect of novel aromatic heterocycle substituted aminamidine derivatives on Necator americanus.

ABSTRACT:

Background

The efficacy of current drugs against hookworms at a single dose is highly variable across regions, age groups and infection intensity. Extensive and repeated use of these drugs also leads to potential drug resistance. Therefore, novel drugs are required for sustained disease control.

Objectives

Novel aromatic heterocycle substituted aminamidine derivatives (AADs) were synthesized based on tribendimine (TBD), and their in vivo potency against Necator americanus was tested.

Methods

The efficacy of the AADs was tested in male hamsters. Oral and IV pharmacokinetic parameters were determined in male Sprague-Dawley rats. The proteomic profiles of N. americanus samples treated with AADs were compared using tandem mass tag-based quantitative proteomic analyses.

SUBMITTER: Huo L 

PROVIDER: S-EPMC11342082 | biostudies-literature | 2024 Jul

REPOSITORIES: biostudies-literature