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Efficient catalytic oxidation of 3-arylthio- and 3-cyclohexylthio-lapachone derivatives to new sulfonyl derivatives and evaluation of their antibacterial activities

Molecules, ISSN: 1420-3049, Vol: 22, Issue: 2
2017
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Article Description

New sulfonyl-lapachones were efficiently obtained through the catalytic oxidation of arylthio- and cyclohexylthio-lapachone derivatives with hydrogen peroxide in the presence of a Mn(III) porphyrin complex. The antibacterial activities of the non-oxidized and oxidized lapachone derivatives against the Gram-negative bacteria Escherichia coli and the Gram-positive bacteria Staphylococcus aureus were evaluated after their incorporation into polyvinylpyrrolidone (PVP) micelles. The obtained results show that the PVP-formulations of the lapachones 4b-g and of the sulfonyl-lapachones 7e and 7g reduced the growth of S. aureus.

Bibliographic Details

Mariana F.Do C. Cardoso; Ana T.P.C. Gomes; Mário M.Q. Simões; Maria G.P.M.S. Neves; José A.S. Cavaleiro; Caroline Dos S. Moreira; David R. Da Rocha; Fernando De C. Da Silva; Vitor F. Ferreira; Catarina Moreirinha; Adelaide Almeida; João Paulo C. Tomé

MDPI AG

Chemistry; Biochemistry, Genetics and Molecular Biology; Pharmacology, Toxicology and Pharmaceutics

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