Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Synthesis and Anti-Paracoccidioides Activity of Calix[n]arenes

Author(s): Marcilene Coimbra de Oliveira, Fabiano Souza Reis, Angelo de Fatima, Thais Furtado Ferreira Magalhaes, Danielle Leticia da Silva, Raphael Rodrigues Porto, Giselle Almeida Watanabe, Cleide Viviane Buzanello Martins, Daniel Leite da Silva, Ana Lucia Tasca Gois Ruiz, Sergio Antonio Fernandes, Joao Ernesto de Carvalho, Maria Aparecida de Resende-Stoianoff.

Abstract:

Fungi are some of the most neglected pathogens in terms of new drug discovery. Paracoccidioidomycosis, an endemic disease to South America, is caused by dimorphic fungi of Paracoccidioides genus. Reasonable citotoxicity, limited efficacy, and frequent use of current commercial antifungals have led to the emergence of resistance. Thus, the development of new antifungals with more selectivity and large spectrum of action is mandatory. In this work, six calix[n]arenes were synthesized and their activity explored against seven isolates of P. brasiliensis and P. lutzii. p-tert- Butylcalix[4]arene (CX1) was the most potent compound against fungal cells and exhibited the lowest toxicity on healthy mammalian cells (V79, hamster lung and MDCK, dog kidney). This is the first report on the effect of calix[n]arenes as growth inhibitors of Paracoccidioides fungi.

Keywords: Calix[n]arenes, P-tert-Butylcalix[n]arene, Antifungal, Paracoccidioides genus, Paracoccidioidomycosis, Dimorphic fungi, Mammalian cells, phenolic, anti-Paracoccidioides, Dimorphic fungus, pathogens, P. brasiliensis, P. lutzii

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Article Details

VOLUME: 9
ISSUE: 1
Year: 2012
Page: [30 - 36]
Pages: 7
DOI: 10.2174/157018012798192991