Title:Synthesis and Antifungal Activity of Coumarins Derivatives Against Sporothrix spp.
VOLUME: 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*
Affiliation:Departamento de Quimica Organica, Universidade Federal Fluminense, Instituto de Quimica, Niteroi, RJ, 24020-150, Universidade Federal do Rio de Janeiro, Instituto de Biofísica 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 Biofísica 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
Keywords:Knoevenagel condensation, addition of thiol, Sporothrix schenckii, Sporothrix brasiliensis, antifungal, synthesis.
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.
