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

Autor:	Faiões Vdos S; Laboratório de Bioquímica de Tripanosomatídeos, Instituto Oswaldo Cruz, Fiocruz, Rio de Janeiro, Brazil., Dos Santos MS; Laboratório de Síntese de Moléculas Bioativas, Instituto de Física e Química, UNIFEI, Itajubá, Minas Gerais, Brazil., Bernardino AM; Programa de Pós-Graduação em Química, Departamento de Química Orgânica, Instituto de Química, UFF, Niterói, Rio de Janeiro, Brazil., Cunha-Júnior EF; Laboratório de Bioquímica de Tripanosomatídeos, Instituto Oswaldo Cruz, Fiocruz, Rio de Janeiro, Brazil., Canto Cavalheiro MM; Laboratório de Bioquímica de Tripanosomatídeos, Instituto Oswaldo Cruz, Fiocruz, Rio de Janeiro, Brazil., Torres-Santos EC; Laboratório de Bioquímica de Tripanosomatídeos, Instituto Oswaldo Cruz, Fiocruz, Rio de Janeiro, Brazil ects@ioc.fiocruz.br.
Jazyk:	angličtina
Zdroj:	Antimicrobial agents and chemotherapy [Antimicrob Agents Chemother] 2014 Oct; Vol. 58 (10), pp. 6290-3. Date of Electronic Publication: 2014 Aug 04.
DOI:	10.1128/AAC.02874-14
Abstrakt:	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. (Copyright © 2014, American Society for Microbiology. All Rights Reserved.)
Databáze:	MEDLINE
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