Zika virus (ZIKV) is a mosquito-borne pathogen which is a current global public health concern. There are currently no approved vaccines or antivirals against ZIKV infection. Taking into account that naphthoquinones have shown promising antiviral activity, the aim of this study was to describe the screening of two bis-naphthoquinones series against ZIKV. Twenty seven compounds were evaluated against ZIKV using Vero cells. The findings showed that among the compounds analyzed four were promising. Compound 3,3’-((2-nitrophenyl)methylene)bis(2-hydroxynaphthalene-1,4-dione) containing the nitro group at the ortho position showed the best selectivity index, followed by compound 3,3’-(4-chlorophenylmethylene)bis(naphthalene-1,2,4-triyl triacetate) with the chlorophenylmethylene radical. These results demonstrate that these bis-naphthoquinones are largely effective in inhibiting the replication of ZIKV.
This paper describes the synthesis and the antileishmanial activity of new pyrazolyl benzenesulfonamide derivatives. These were elucidated by spectrometric methods. Some compounds showed a significant in vitro activity against Leishmania amazonensis, highlighting the derivative 1e. These pyrazolyl benzenesulfonamide derivatives did not show any toxicity in murine macrophage.
Este artigo descreve a síntese e a atividade antileishmania de novos derivados pirazolil benzenossulfonamídicos. Estes foram elucidados por métodos espectrométricos. Alguns compostos mostraram uma atividade in vitro significativa contra Leishmania amazonensis, destacando-se o derivado 1e. Nenhum dos derivados pirazolil benzenossulfonamídicos mostraram qualquer toxicidade em macrófagos murinos.
We describe a mild and efficient method for the formation of 3-(2'-aminoaryl)pyrazoles in excellent yields from reactions of 4-chloroquinolines with hydrazine. These heterocyclic ring opening reactions occur under much milder conditions then previously described.
Um método mais suave e eficiente é descrito para a síntese de 3-(2'-aminoaril)pirazóis, a partir das reações de 4-cloroquinolinas com hidrazina em excelentes rendimentos. Estas reações de abertura de anel heterocíclico ocorrem em condições mais suaves do que as descritas anteriormente.