resumo
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.
palavras-chave
TRYPANOSOMA-CRUZI ACTIVITY; NOR-BETA-LAPACHONE; ORGANOSULFUR COMPOUNDS; ANTITUMOR-ACTIVITY; NAPHTHOQUINONES; COMPLEXES; AGENTS; PORPHYRINS; PARAMETERS; DELIVERY
categoria
Chemistry
autores
Cardoso, MFD; Gomes, ATPC; Moreira, CD; Simoes, MMQ; Neves, MGPMS; da Rocha, DR; da Silva, FD; Moreirinha, C; Almeida, A; Ferreira, VF; Cavaleiro, JAS
nossos autores
agradecimentos
The authors would like to acknowledge the agencies that fund our research: CNPq, CAPES and FAPERJ, particularly through project funding PRONEX-FAPERJ (E-26/110.574/2010). Thanks are also due to FCT (Portugal), the European Union, QREN, FEDER and COMPETE for funding the research unit QOPNA (project PEstC/QUI/UI0062/2011), CESAM (FCT UID/MAR/0017/2013), the National NMR Network, and the project QREN (FCOMP-01-0124-FEDER-010840) (PTDC/QUI-QUI/102454/2008). Thanks are also due to the protocol agreement CAPES- FCT. Mariana F. C. Cardoso thanks CAPES for her scholarship (process 7129/13-0)). Ana Gomes thanks FCT for her post-doctoral fellowship (SFRH/BPD/79521/2011). Catarina Moreirinha gives thanks her postdoctoral grant (LIFE13 ENV/ES/001048).