Synthesis And Antifungal Activity of Coumarins Derivatives against Sporothrix spp.

Synthesis And Antifungal Activity of Coumarins Derivatives against Sporothrix spp.

Curr Top Med Chem. 2018 Feb 20;:

Authors: Forezi LSM, Borba-Santos LP, Cardoso MFC, Ferreira VF, Rozental S, Da Silva FC

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 active compounds were 16b and 17i. These compounds inhibited fungal growth at 31.25 µM (minimum inhibitory concentration) and kill both species up to 500 µM (minimum fungicidal concentration). Thus, 16b and 17i exhibited good antifungal activity against S. brasiliensis and S. schenckii, suggesting that they are important scaffolds for development of novel antifungal agents.

PMID: 29473510 [PubMed - as supplied by publisher]

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