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The in vitro antifungal activity of some dithiocarbamate organotin(IV) compounds on Candida albicans - a model for biological interaction of organotin complexes

机译:某些二硫代氨基甲酸酯有机锡(IV)化合物对白色念珠菌的体外抗真菌活性-有机锡复合物生物相互作用的模型

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摘要

The in vitro antifungal activity of the dithiocarbamate organotin complexes [Sn{S2CN(CH2)4}2Cl2] (1), [Sn{S2CN(CH2)4)2Ph2] (2), [Sn{S2CN(CH2)4}Ph3] (3), [Sn{S2CN(CH2)4}2n-Bu2] (4), [Sn{S2CN(CH2)4}Cy3] {Cy = cyclohexyl} (5), [Sn{S2CN(C2Hs)2}2Cl2] (6), [Sn(S2CN(C2H5)2}2Ph2] (7), [Sn{S2CN(C2H5)2lPh3] (8), [Sn{S2CN(C2H5)2}3Ph] (9) and [Sn{S2CN(C2H5)2}Cy3] (10) has been screened against Candida albicans (ATCC 18804), Candida tropicalis (ATCC 750) and resistant Candida albicans collected from HIV-positive Brazilian patients with oral candidiasis. All compounds exhibited antifungal activities and complexes 3 and 8 displayed the best results. We have investigated the effect of compounds 1 -10 on the cellular activity of the yeast cultures. Changes in mitochondrial function have not been detected. However, all drugs reduced ergosterol biosynthesis. Preliminary studies on DNA integrity indicated that the compounds do not cause gross damage to yeast ONA. The data suggest that these compounds share some mechanisms of action on cell membranes similar to that of polyene but not with azole drugs, normally used in Candida infections.
机译:二硫代氨基甲酸酯有机锡复合物[Sn {S2CN(CH2)4} 2Cl2](1),[Sn {S2CN(CH2)4)2Ph2](2),[Sn {S2CN(CH2)4} Ph3的体外抗真菌活性](3),[Sn {S2CN(CH2)4} 2n-Bu2](4),[Sn {S2CN(CH2)4} Cy3] {Cy =环己基}(5),[Sn {S2CN(C2Hs)2] } 2Cl2](6),[Sn(S2CN(C2H5)2} 2Ph2](7),[Sn {S2CN(C2H5)2lPh3](8),[Sn {S2CN(C2H5)2} 3Ph](9)和[Sn {S2CN(C2H5)2} Cy3](10)已针对白色念珠菌(ATCC 18804),热带念珠菌(ATCC 750)和从口腔感染念珠菌病的艾滋病毒呈阳性的巴西患者中收集的耐药白色念珠菌进行了筛选。所有化合物均表现出抗真菌作用活性和复合物3和8表现出最好的结果,我们已经研究了化合物1 -10对酵母培养物的细胞活性的影响,尚未检测到线粒体功能的变化,但是,所有药物都降低了麦角固醇的生物合成。 DNA完整性表明这些化合物不会对酵母ONA造成严重损害,数据表明这些化合物应在细胞膜上的某些作用机制与多烯类似,但对念珠菌感染通常不使用的唑类药物起作用。

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