Evaluating 5-Nitrothiazoles as Trypanocidal Agents-Reference-Cited by-同舟云学术

Evaluating 5-Nitrothiazoles as Trypanocidal Agents

Published:2016-02 Issue:2 Volume:60 Page:1137-1140
ISSN:0066-4804
Container-title:Antimicrobial Agents and Chemotherapy
language:en
Short-container-title:Antimicrob Agents Chemother

Author:

O'Shea Ivan P.¹,Shahed Mohammed¹,Aguilera-Venegas Benjamín²,Wilkinson Shane R.¹

Affiliation:

1. School of Biological and Chemical Sciences, Queen Mary University of London, London, United Kingdom

2. Laboratory of Antioxidants, Institute of Nutrition and Food Technology, University of Chile, Santiago, Chile

Abstract

ABSTRACT The growth-inhibitory properties of a 5-nitrothiazole series were evaluated against Trypanosoma brucei . A subset of related compounds displayed the greatest potency toward the parasite while exhibiting little cytotoxic effect on mammalian cells, with this antiparasitic activity dependent on expression of a type I nitroreductase by the trypanosome. We conclude that the 5-nitrothiazole class of nitroheterocyclic drugs may represent a new lead in the treatment of human African trypanosomiasis.

Funder

Fondo Nacional de Desarrollo Cientifico y Tecnologico

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

Link

https://journals.asm.org/doi/pdf/10.1128/AAC.02006-15

Reference20 articles.

1. Human African trypanosomiasis

2. Trypanocidal drugs: mechanisms, resistance and new targets

3. Nifurtimox-eflornithine combination therapy for second-stage African Trypanosoma brucei gambiense trypanosomiasis: a multicentre, randomised, phase III, non-inferiority trial