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[3-甲硫基-、3-(氨基取代)乙硫基-、3-羧甲基硫基-、3,3'-(二硫代双)-5-芳基-4H(R)-1,2,4-三唑以及5-芳基-4H(R)-1,2,4-三唑啉-3-硫酮的2-氨甲基-N-取代衍生物:合成与生物活性]

[3-Methylthio-, 3-(amino-substituted)ethylthio-, 3-carboxymethylthio-, 3,3'-(dithiobis)-5-aryl-4H(R)-1,2,4-triazoles and 2-aminomethyl-N-substituted derivatives of 5-aryl-4H(R)-1,2,4-triazolin-3-thione: synthesis and biological activity].

作者信息

Mazzone G, Bonina F, Blandino G

出版信息

Farmaco Sci. 1981 Dec;36(12):1004-18.

PMID:7319022
Abstract

Following previous research which showed the antibacterial and antimycotic activity of triazolin-3-thiones (II), a series of compounds has been prepared and tested to correlate and clarify the structure-activity relationships. The compounds were of the type represented in (II) where (R = H, CH3 or C6H5) and were in detail: 3-methylthiotriazoles (III-VIII), 3-(amino-substituted)ethylthiotriazolines (IX-XXVI), 3-carboxymethylthiotriazolines (XXVII-XXX), 3,3'dithiobistriazolines (XXXI-XXXVI) and 2-amino-methyl-N-substituted triazolin-3-thiones (XLVIII-LXVI). The 2-aminooxadiazoles (XXXVII-XLII), obtained in place of the expected 1-aroyl-S-methylisothiosemicarbazides (II a) from the reaction between thiosemicarbazides (I) (R = H; CH3, C6H5) and methyl iodide, are also described.

摘要

先前的研究表明三唑啉-3-硫酮(II)具有抗菌和抗真菌活性,在此基础上,制备并测试了一系列化合物,以关联和阐明构效关系。这些化合物为(II)所示类型,其中(R = H、CH₃或C₆H₅),具体如下:3-甲基硫代三唑(III - VIII)、3-(氨基取代)乙基硫代三唑啉(IX - XXVI)、3-羧甲基硫代三唑啉(XXVII - XXX)、3,3'-二硫代双三唑啉(XXXI - XXXVI)和2-氨基甲基-N-取代三唑啉-3-硫酮(XLVIII - LXVI)。还描述了由硫代氨基脲(I)(R = H;CH₃、C₆H₅)与碘甲烷反应得到的2-氨基恶二唑(XXXVII - XLII),它们取代了预期的1-芳酰基-S-甲基异硫脲(II a)。

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