Yu Shichong

The design, synthesis and bioimaging of main group elements substituted near-infrared fluorescent rhodamine dyes and probes

Near Infrared (NIR) fluorescence imaging is significant in bioimaging with many favorable characteristics, including high signal/noise ratio, deep penetration and low photo-toxicity. The main group elements substituted rhodamine dyes have attracted large attention not only due to the NIR characteristics, but also many inherited outstanding merits of rhodamine dyes. Among the developed rhodamine dyes, the dyes whose bridging oxygen are substituted by silicon have attracted most interests and been widely used in the fluorescence bioimaging. The development of NIR main group elements substituted rhodamine dyes has enriched the species and quantity of the fluorescent probes and enlarged their application. Herein we reviewed the design, development and application of main group substituted rhodamine in recent years.

Design, synthesis, and antifungal activity of 3-substituted triazole derivatives.

Objective To study the in vitro antifungal activity of triazole alcohols by introduction of 1,2,3-triazole as the side chain.Methods Twenty-one novel triazole alcohol compounds were designed,synthesized,and characterized by 1 HNMR and MS spectra.The in vitro antifungal activities of the compounds were evaluated using eight kinds of pathogenic fungi.Results All the synthesized compounds exhibited certain antifungal activities.The MIC80value of compound7 1-(1 H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-[N,N-(1-substituted-benzyl-4-methylene-1 H-1,2,3-triazole)]against Candida albicans was 0.25μg/ml,with its activity being 4times that of fluconazole.The MIC80value of compoundⅥ1-(1 H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-(N,N-dipropargyl)-2-propanols against Candida albicans was 0.015 6μg/ml,with its activity being 64times that of fluconazole and 4times that of itraconazole.Conclusion The 1,2,3-triazole can be efficiently introduced by intermolecular 1,3-dipolar cycloaddition.Large side chains may be a disadvantage for improving the antifungal activity of the title compounds.