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

Viviane dos Santos Faiões | Zendy; Maurício Silva dos Santos | Zendy; Alice M. R. Bernardino | Zendy; Edézio Ferreira CunhaJúnior | Zendy; Marilene Marcuzzo do Canto Cavalheiro | Zendy; Eduardo Caio Torres-Santos | Zendy

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

Author(s) -

Viviane dos Santos Faiões,

Maurício Silva dos Santos,

Alice M. R. Bernardino,

Edézio Ferreira CunhaJúnior,

Marilene Marcuzzo do Canto Cavalheiro,

Eduardo Caio Torres-Santos

Publication year - 2014

Publication title -

antimicrobial agents and chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.07

H-Index - 259

eISSN - 1070-6283

pISSN - 0066-4804

DOI - 10.1128/aac.02874-14

Subject(s) - leishmaniasis , pharmacology , allopurinol , cutaneous leishmaniasis , amastigote , amphotericin b , leishmania mexicana , medicine , leishmania , immunology , parasite hosting , dermatology , antifungal , world wide web , computer science

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.

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