alexa Phebalosin and its Structural Modifications are Active
ISSN: 2161-0444

Medicinal chemistry
Open Access

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Research Article

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

Fabiana C Missau1,4, Susana Johann2*, Nívea Pereira de Sá2, Patrícia S Cisalpino2, Carlos A Rosa2, Beatriz A Ferreira3 and Moacir G Pizzolatti1

1Departamento de Química, Universidade Federal de Santa Catarina, CEP 88040-970, Florianópolis, SC, Brazil

2Departamento de Microbiologia, Universidade Federal de Minas Gerais, CEP 31270-901, Belo Horizonte, MG, Brazil

3Campus Centro Oeste Dona Lindu, Universidade Federal de São João Del Rei, CEP 35501-296, Divinópolis, MG, Brazil

4Campus Itaqui, Universidade Federal do Pampa (UNIPAMPA), CEP 97650-000, Itaqui, RS, Brazil

*Corresponding Author:
Susana Johann
Departamento de Microbiologia
Instituto de Ciências Biológicas
Universidade Federal de Minas Gerais
Av. Antônio Carlos, 6627, PO Box 486
31270-901, Belo Horizonte, MG, Brazil
Tel: +55 3349 7700
Fax: +55 31 3295 3115
E-mail: [email protected]

Received date: June 18, 2014; Accepted date: July 28, 2014; Published date: July 30, 2014

Citation: FC, Johann S, de Sá NP, Cisalpino PS, Rosa CA, et al. (2014) Phebalosin and its Structural Modifications are Active against the Pathogenic Fungal Causing Paracoccidioidomycosis. Med chem 4:581-587. doi:10.4172/2161-0444.1000197

Copyright: © 2014 Missau FC, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

 

Abstract

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.

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