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具有预期生物活性的4(H)-1,2,4-三唑衍生物。

4(H)-1,2,4-triazole derivatives with expected biological activity.

作者信息

Lange J, Tondys H

出版信息

Pol J Pharmacol Pharm. 1975 Apr-Jun;27(2):203-9.

PMID:1153352
Abstract

Three isomeric 4-(carboxyphenyl)-3,5-diphenyl-1,2,4-triazoles (III) were prepared by condensation of bis(alpha-chlorobenzylidene)hydrazine (I) with ethyl aminobenzoate and subsequent alkaline hydrolysis of the ethyl esters (II) of III. III were also obtained by hydrolysis of the cyano compounds (IV) and by oxidation of the methyl derivatives (VI). A similar condensation of I with aminopyridines led to 4-pyridyl-3,5-diphenyl-1,2,4-triazoles (VII). Reduction of three isomeric 4-(nitrophenyl)-3,5-diphenyl-1,2,4-triazoles (X) (Fe/AcOH) gave the corresponding amino derivatives (XI). In the preparation of X, the method employing N-(nitrophenyl)-benzimidoyl chloride (VIII) and benzhydrazide (IX) proved to be most advantageous. Slight bacteriostatic activity of the triazoles prepared was observed in standard in vitro tests.

摘要

通过双(α-氯亚苄基)肼(I)与氨基苯甲酸乙酯缩合,随后对III的乙酯(II)进行碱性水解,制备了三种异构体4-(羧基苯基)-3,5-二苯基-1,2,4-三唑(III)。III也可通过氰基化合物(IV)的水解和甲基衍生物(VI)的氧化得到。I与氨基吡啶的类似缩合反应生成了4-吡啶基-3,5-二苯基-1,2,4-三唑(VII)。三种异构体4-(硝基苯基)-3,5-二苯基-1,2,4-三唑(X)(铁/乙酸)还原得到相应的氨基衍生物(XI)。在制备X时,采用N-(硝基苯基)-苯甲酰氯(VIII)和苯肼(IX)的方法被证明是最有利的。在标准体外试验中观察到所制备的三唑具有轻微的抑菌活性。

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