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LeishmanicidalActivities of NovelSynthetic Furoxan andBenzofuroxanDerivatives Luiz Antônio DutraLetícia de AlmeidaThaís G. Passalacqua2014 год

Leishmanicidal Activities of Novel Synthetic Furoxan and Benzofuroxan Derivatives
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Аннотация: ABSTRACT A novel series of furoxan (1,2,5-oxadiazole 2-oxide) (compounds 3, 4a and -b, 13a and -b, and 14a to -f) and benzofuroxan (benzo[c][1,2,5]oxadiazole 1-oxide) (compounds 7 and 8a to -c) derivatives were synthesized, characterized, and evaluated for in vitro activity against promastigote and intracellular amastigote forms of Leishmania amazonensis . The furoxan derivatives exhibited the ability to generate nitric oxide at different levels (7.8% to 27.4%). The benzofuroxan derivative 8a was able to increase nitrite production in medium supernatant from murine macrophages infected with L. amazonensis at 0.75 mM after 48 h. Furoxan and benzofuroxan derivatives showed remarkable leishmanicidal activity against both promastigote and intracellular amastigote forms. Compounds 8a, 14a and -b, and 14d exerted selective leishmanicidal activities superior to those of amphotericin B and pentamidine. In vitro studies at pH 5.4 reveal that compound 8a is stable until 8 h and that compound 14a behaves as a prodrug, releasing the active aldehyde 13a. These compounds have emerged as promising novel drug candidates for the treatment of leishmaniasis.
Год издания: 2014
Авторы: Luiz Antônio Dutra, Letícia de Almeida, Thaís G. Passalacqua, Juliana Santana Reis, Fábio Aurélio Esteves Torres, Isabel Martínez, Rosângela Gonçalves Peccinini, Chung Man Chin, Konstantin Chegaev, Stefano Guglielmo, Roberta Fruttero, Márcia A. S. Graminha, Jean Leandro dos Santos
Издательство: American Society for Microbiology
Источник: Antimicrobial Agents and Chemotherapy
Ключевые слова: Research on Leishmaniasis Studies, Synthesis and Biological Evaluation, Insect Pest Control Strategies
Другие ссылки: Antimicrobial Agents and Chemotherapy (PDF)
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Institutional Research Information System University of Turin (University of Turin) (PDF)
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Acervo Digital da Universidade Estadual Paulista (Universidade Estadual Paulista) (PDF)
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