| Literature DB >> 25092697 |
Viviane Dos Santos Faiões1, Maurício Silva Dos Santos2, Alice Maria Rolim Bernardino3, Edézio Ferreira Cunha-Júnior1, Marilene Marcuzzo do Canto Cavalheiro1, Eduardo Caio Torres-Santos4.
Abstract
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.Entities:
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Year: 2014 PMID: 25092697 PMCID: PMC4187983 DOI: 10.1128/AAC.02874-14
Source DB: PubMed Journal: Antimicrob Agents Chemother ISSN: 0066-4804 Impact factor: 5.191