The trifluoromethoxy(CF_3O) group has become a novel moiety in various fields because of its unique features. However, despite the promising applications, the synthesis of CF_3O-containing compounds is still a challen...The trifluoromethoxy(CF_3O) group has become a novel moiety in various fields because of its unique features. However, despite the promising applications, the synthesis of CF_3O-containing compounds is still a challenge due to indirect synthetical strategies and volatile reagent which is hard to handle. Until very recently, several innovative reagents were developed to facilitate the trifluoromethoxylation reaction and make CF_3O-containing compounds more accessible. This review mainly focuses on the recent advances in new trifluoromethoxylation reagents and their usage.展开更多
A series of five new Schiff bases(1–5) were synthesized by reacting 2-(trifluoromethoxy) aniline with different aromatic aldehydes. The Schiff base compounds were characterized by spectroscopic and analytical methods...A series of five new Schiff bases(1–5) were synthesized by reacting 2-(trifluoromethoxy) aniline with different aromatic aldehydes. The Schiff base compounds were characterized by spectroscopic and analytical methods. Crystal structure of one new compound was also reported. The pharmacological properties, including antibacterial(14 bacterial species), antifungal(7 strains), antimalarial, anti-trypanosomal and anti-HIV activities of the compounds, were investigated. Cytotoxicity of the tested compounds was evaluated against human cervix adernocarcinoma cells(He La). Bacterial minimum inhibitory concentration(MIC) results by broth microdilution method showed that Bacillus subtilis, Enterococcus faecalis, Staphylococcus aureus, Staphylococcus epidermidis, Proteus vulgaris, Klebsiella oxytoc and Klebsiella pneumonia were more sensitive in the presence of tested compounds with an MIC value of 15.6 μg/m L. All the tested compounds showed good to moderate activity against fungi. The sensitivity of Aspergillus fumigatus was higher than other strains with a minimum cell death concentration(MFC) of 15.6 μg/m L. Compound 1 showed greater antimalarial and anti-trypanosomal properties with very low to no cytotoxic effects against He La cells as compared with compound 5, while other compounds exhibited poor activity. Compounds 1–5 demonstrated good activity against HIV type-1. These Schiff base compounds could be used as good antimicrobial agents.展开更多
基金supported by the National Key Research and Development Program of China(2016YFA0602900)the National Natural Science Foundation of China(21522205,21672110)the Fundamental Research Funds for the Central Universities
文摘The trifluoromethoxy(CF_3O) group has become a novel moiety in various fields because of its unique features. However, despite the promising applications, the synthesis of CF_3O-containing compounds is still a challenge due to indirect synthetical strategies and volatile reagent which is hard to handle. Until very recently, several innovative reagents were developed to facilitate the trifluoromethoxylation reaction and make CF_3O-containing compounds more accessible. This review mainly focuses on the recent advances in new trifluoromethoxylation reagents and their usage.
文摘A series of five new Schiff bases(1–5) were synthesized by reacting 2-(trifluoromethoxy) aniline with different aromatic aldehydes. The Schiff base compounds were characterized by spectroscopic and analytical methods. Crystal structure of one new compound was also reported. The pharmacological properties, including antibacterial(14 bacterial species), antifungal(7 strains), antimalarial, anti-trypanosomal and anti-HIV activities of the compounds, were investigated. Cytotoxicity of the tested compounds was evaluated against human cervix adernocarcinoma cells(He La). Bacterial minimum inhibitory concentration(MIC) results by broth microdilution method showed that Bacillus subtilis, Enterococcus faecalis, Staphylococcus aureus, Staphylococcus epidermidis, Proteus vulgaris, Klebsiella oxytoc and Klebsiella pneumonia were more sensitive in the presence of tested compounds with an MIC value of 15.6 μg/m L. All the tested compounds showed good to moderate activity against fungi. The sensitivity of Aspergillus fumigatus was higher than other strains with a minimum cell death concentration(MFC) of 15.6 μg/m L. Compound 1 showed greater antimalarial and anti-trypanosomal properties with very low to no cytotoxic effects against He La cells as compared with compound 5, while other compounds exhibited poor activity. Compounds 1–5 demonstrated good activity against HIV type-1. These Schiff base compounds could be used as good antimicrobial agents.
