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Synthesis and Antifungal Activity of Coumarins Derivatives Against Sporothrix spp.

[ Vol. 18 , Issue. 2 ]

Author(s):

Luana da S.M. Forezi, Luana Pereira Borba-Santos, Mariana F.C. Cardoso, Vitor F. Ferreira, Sonia Rozental and Fernando de C. da Silva*   Pages 164 - 171 ( 8 )

Abstract:


Sporotrichosis is a serious public health problem in Brazil that affects human patients and domestic animals, mainly cats. Thus, the search for new antifungal agents is required also due to the emergence and to the lack of effective drugs available in the therapeutic arsenal. The aim of this study was to evaluate the in vitro antifungal profile of two synthetic series of coumarin derivatives against Sporothrix schenckii and Sporothrix brasiliensis. The three-components synthetic routes used for the preparation of coumarin derivatives have proved to be quite efficient and compounds 16 and 17 have been prepared in good yields. The inhibitory activity of nineteen synthetic coumarins derivatives 16a-i and 17a-j were evaluated against Sporothrix spp. yeasts and the most potent compounds were 16b and 17i. However, according to concentrations able to inhibit (minimum inhibitory concentrations) and kill (minimum fungicidal concentrations) the cells, 17i was more effective than 16b against Sporothrix spp. Thus, 17i exhibited good antifungal activity against S. brasiliensis and S. schenckii, suggesting that it is an important scaffold for the development of novel antifungal agents.

Keywords:

Knoevenagel condensation, addition of thiol, Sporothrix schenckii, Sporothrix brasiliensis, antifungal, synthesis.

Affiliation:

Departamento de Quimica Organica, Universidade Federal Fluminense, Instituto de Quimica, Niteroi, RJ, 24020-150, Universidade Federal do Rio de Janeiro, Instituto de BiofĂ­sica Carlos Chagas Filho, Cidade Universitaria, Rio de Janeiro, RJ, 21941-901, Departamento de Quimica Organica, Universidade Federal Fluminense, Instituto de Quimica, Niteroi, RJ, 24020-150, Universidade Federal Fluminense, Departamento de Tecnologia Farmaceutica, Faculdade de Farmacia, Niteroi, RJ, 24241-002, Universidade Federal do Rio de Janeiro, Instituto de BiofĂ­sica Carlos Chagas Filho, Cidade Universitaria, Rio de Janeiro, RJ, 21941-901, Departamento de Quimica Organica, Universidade Federal Fluminense, Instituto de Quimica, Niteroi, RJ, 24020-150

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