The new pyrazolyltetrazole derivative MSN20 is effective via oral delivery against cutaneous leishmaniasis

An orally delivered, safe and effective treatment for leishmaniasis is an unmet medical need. Azoles and the pyrazolylpyrimidine allopurinol present leishmanicidal activity, but their clinical efficacies are variable. Here, we describe the activity of the new pyrazolyltetrazole hybrid, 5-[5-amino-1-...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:Antimicrobial agents and chemotherapy 2014-10, Vol.58 (10), p.6290-6293
Hauptverfasser: Faiões, Viviane Dos Santos, Dos Santos, Maurício Silva, Bernardino, Alice Maria Rolim, Cunha-Júnior, Edézio Ferreira, Canto Cavalheiro, Marilene Marcuzzo do, Torres-Santos, Eduardo Caio
Format: Artikel
Sprache:eng
Schlagworte:
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:An orally delivered, safe and effective treatment for leishmaniasis is an unmet medical need. Azoles and the pyrazolylpyrimidine allopurinol present leishmanicidal activity, but their clinical efficacies are variable. Here, we describe the activity of the new pyrazolyltetrazole hybrid, 5-[5-amino-1-(4'-methoxyphenyl)1H-pyrazole-4-yl]1H-tetrazole (MSN20). MSN20 showed a 50% inhibitory concentration (IC50) of 22.3 μM against amastigotes of Leishmania amazonensis and reduced significantly the parasite load in infected mice, suggesting its utility as a lead compound for the development of an oral treatment for leishmaniasis.
ISSN:0066-4804
1098-6596
DOI:10.1128/AAC.02874-14