Pyrazoline derivatives as promising novel antischistosomal agents

Autor: Cristiane S. Morais, Ana C. Mengarda, Fábio B. Miguel, Karine B. Enes, Vinícius C. Rodrigues, Maria Cristina C. Espírito-Santo, Abolghasem Siyadatpanah, Polrat Wilairatana, Mara R. C. Couri, Josué de Moraes
Jazyk: angličtina
Rok vydání: 2021
Předmět:
Zdroj: Scientific Reports, Vol 11, Iss 1, Pp 1-13 (2021)
Druh dokumentu: article
ISSN: 2045-2322
DOI: 10.1038/s41598-021-02792-0
Popis: Abstract Praziquantel is the only available drug to treat schistosomiasis, a parasitic disease that currently infects more than 240 million people globally. Due to increasing concerns about resistance and inadequate efficacy there is a need for new therapeutics. In this study, a series of 17 pyrazolines (15–31) and three pyrazoles (32–34) were synthesized and evaluated for their antiparasitic properties against ex vivo adult Schistosoma mansoni worms. Of the 20 compounds tested, six had a 50% effective concentration (EC50) below 30 μM. Our best hit, pyrazoline 22, showed promising activity against adult schistosomes, with an EC50
Databáze: Directory of Open Access Journals