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某些3-(2-苯乙基)-5-取代-四氢-2H-1,3,5-噻二嗪-2-硫酮的合成及其抗真菌活性

Syntheses and antifungal activities of some 3-(2-phenylethyl)-5-substituted- tetrahydro-2H-1,3,5-thiadiazine-2-thiones.

作者信息

Ertan M, Bilgin A A, Palaska E, Yulug N

机构信息

Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Hacettepe University, Ankara, Turkey.

出版信息

Arzneimittelforschung. 1992 Feb;42(2):160-3.

PMID:1610428
Abstract

Ten new 3-(2-phenethyl)-5-substituted-tetrahydro-2H-1,3,5-thiadiazine-2- thiones were synthesized by the reaction of phenylethylamine with carbon disulfide and potassium hydroxide, followed by formaldehyde and appropriate amino acids. The structures of these compounds have been confirmed by UV, IR, 1H-NMR and elementary analysis. The antifungal activities of the compounds were tested by tube dilution method against yeast-like fungi (Candida albicans, C. parapsilosis, C. stellatoidea and C. pseudotropicalis) and minimal inhibitory concentration (MIC) and minimal fungicidal concentration (MFC) values were determined. All compounds proved to be highly effective against yeast-like fungi (MFC range: 1.56-12.5 micrograms/ml).

摘要

通过苯乙胺与二硫化碳和氢氧化钾反应,然后与甲醛和适当的氨基酸反应,合成了十种新的3-(2-苯乙基)-5-取代-四氢-2H-1,3,5-噻二嗪-2-硫酮。这些化合物的结构已通过紫外光谱、红外光谱、¹H-核磁共振谱和元素分析得到证实。采用试管稀释法对这些化合物针对酵母样真菌(白色念珠菌、近平滑念珠菌、星状念珠菌和伪热带念珠菌)的抗真菌活性进行了测试,并测定了最低抑菌浓度(MIC)和最低杀菌浓度(MFC)值。所有化合物均被证明对酵母样真菌具有高效性(MFC范围:1.56-12.5微克/毫升)。

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