A series of phenylbipyridinylpyrazoles was synthesized through the reaction of 2-(4-(2-chloropyridin-4-yl)-3-(3-methoxy-5-methylphenyl)-1H-pyrazol-1-yl)acetonitrile (4) with different 6-substituted pyridine-3-ylboronic acids. The final compounds 5a-j were screened at 10 µM against over 60 tumor cell lines at the U.S. National Cancer Institute (NCI). In light of the NCI results, compounds 5c and...

Leishmaniasis remains a serious public health problem in developing countries without effective control, whether by vaccination or chemotherapy. Part of the failure of leishmaniasis control is due to the lack of new less toxic and more effective drugs able to eliminate both the lesions and the parasite. Oxiranes derived from naphthoquinones now being assayed are promising drugs for the treatmen...

The phenyliodonium ylide of 2-hydroxy-1,4-naphthoquinone reacts with aminoesters, ureas, aminoalcohols and aminophenols in refluxing dichloromethane to afford good yields of indanedione 2-carboxamido compounds, that in solution exist in an enol-amide form. The same reactants in a copper-catalyzed reaction afford mainly the corresponding N-arylo compounds. Arylhydrazines are mainly oxidized by t...

Objective: Presently, one of the most common oral diseases is dental caries, which a biofilm-mediated disease. Lawsone methyl ether (LME) has shown promising antibacterial activity due to its 1,4-napthoquinone structure. Recently, 1,2,3-triazole scaffold been used in structural modification potential antimicrobial agents. To develop novel anticaries agents, structure with N-substituted 1,2,3-tr...

Impatiens balsamina L. (Balsaminaceae), an annual herb found throughout China, has been extensively used in traditional Chinese medicine (TCM). However, our knowledge regarding the adverse effects of I. balsamina in vivo is very limited. In this present study, the nematode Caenorhabditis elegans model was employed to fully assess the adverse effects of hydroalcoholic (EtOH 55%) extracts of I. b...

The complexation equi li bria of zinc(lI ) wi th 2-hydroxy-IAnaphthoquinone. 5-hydroxyIA-naphthoquinone and 5.8-dihydroxyIA-naphthoquinone have been studied spectrophotometri call y as a function of pH in 50~ (1'/1') ethanol-water medium at 25°C and an ionic strength of 0.1 M NaCI04 . The spectral study of the complexati on reactions has been carried out in solutions contain ing equimolar conce...

The toxic profile of lawsone (2-hydroxy-[1,4]naphthoquinone) and a series of [1,4]naphthoquinone derivatives was evaluated against the brine shrimp Artemia salina and against the mollusk Biomphalaria glabrata, the main transmitting vector of schistosomiasis in Brazil. Of the seventeen compounds tested nine fell below the threshold of 100 microg/mL set for potential molluscicidal activity by the...

incorporation of this acid in vitamin K 2 23 and vitamin K t 4 in bacteria and higher plants. Degradation of labeled vitamin K 2 after feeding shikimic acid (-U-1 4C) has shown that the intact ring of this acid is incorporated into the benzenoid moiety of this naphthoquinone 2 ' 3 . fn contrast, the degradation studies on lawsone 1 indicated that the ring atoms of shikimic acid (-U-1 4C) are tr...

INTRODUCTION Naphthoquinone derivatives are under investigation as potential therapeutic agents. The antibacterial and antifungal activity of lawsone and of some novel naphthoquinone derivatives was assessed in vitro. METHODS The antimicrobial activity was determined using diffusion disk and the broth microdilution methods against seven bacteria and three Candida species, according to recomme...