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American Society for Microbiology, Antimicrobial Agents and Chemotherapy, 10(58), p. 6290-6293, 2014

DOI: 10.1128/aac.02874-14

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The New Pyrazolyltetrazole Derivative MSN20 Is Effective via Oral Delivery against Cutaneous Leishmaniasis

Journal article published in 2014 by Marilene Marcuzzo do Canto Cavalheiro, Maurício Silva dos Santos, Viviane Dos Santos Faiões, Eduardo Caio Torres-Santos, A. Maria Rolim Bernardino ORCID, Maurício Silva Dos Santos, Alice Maria Rolim Bernardino, E. Ferreira Cunha-Júnior, Edézio Ferreira Cunha-Júnior, M. Marcuzzo Canto Cavalheiro, Marilene Marcuzzo do Canto Cavalheiro, E. Calo Torres-Santos
This paper is made freely available by the publisher.
This paper is made freely available by the publisher.

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Abstract

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 (IC 50 ) 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.