Chimie médicale

Phebalosin and its Structural Modifications are Active against the Pathogenic Fungal Causing Paracoccidioidomycosis

Abstract

Fabiana C Missau, Susana Johann, Nívea Pereira de Sá, Patrícia S Cisalpino, Carlos A Rosa, Beatriz A Ferreira and Moacir G Pizzolatti

The phebalosin was isolated from hexane extract of the Polygala paniculata (Polygalaceae). The structural modifications of phebalosin were performed on the epoxy group with different nucleophiles such as H2O, ethoxy, methoxy, isopropoxy and n-butoxy for the corresponding derivatives and with acetic   fungus Paracoccidioides brasiliensis. In this work phebalosin showed promised antifungal activity against isolates of P. brasiliensis with MIC value of 31.2 and 62.5 μg/ml. The compound 3 presented the better activity with MIC value of 1.9 μg/ml gainst the isolate P. brasiliensis Pb03. Besides, it was used methods of theoretical Chemistry, and chemometrics analysis techniques to perform a SAR study. The compounds activity is due to both types of properties – electronic and structural ones. Overall, these data open new possibilities for the potential use of phebalosin and its structural modifications as antifungal.