首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis, characterization and derivatization of some novel types of mono- and bis-imidazolidineiminothiones and imidazolidineiminodithiones with antitumor, antiviral, antibacterial and antifungal activities--part I.
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Synthesis, characterization and derivatization of some novel types of mono- and bis-imidazolidineiminothiones and imidazolidineiminodithiones with antitumor, antiviral, antibacterial and antifungal activities--part I.

机译:具有抗肿瘤,抗病毒,抗菌和抗真菌活性的一些新型单-和双-咪唑烷亚胺基硫酮和咪唑烷亚氨基二硫酮的合成,表征和衍生化-第一部分。

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摘要

Halogenated and alkylated N-arylcyanothioformanilides were reacted with the nucleophilic reagents triethylamine, hydrazine and diphenyldiazomethane to produce N-arylcyanothioformanilide ammonium salts, a thiosemicarbazide and a 2-(arylamino)-3,3-diphenylacrylonitrile, respectively. They also underwent several types of electrophilic reactions with aryl-, arylbisisocyanates and arylisothiocyanates to yield mono- and bis-imidazolidineiminothiones and imidazolidineiminodithiones. Treatment of imidazolidineiminothiones with hydrogen sulfide, substituted ortho-phenylenediamines and thiocarbohydrazide afforded the corresponding thiohydantoin, quinoxaline and imidazotriazine derivatives. Several of the synthesized products were subjected to in vitro biological evaluation against antitumor, antiviral, antimicrobial and antifungal strains. Most tested compounds showed significant activities.
机译:使卤代和烷基化的N-芳基氰基硫代甲酰苯胺与亲核试剂三乙胺,肼和二苯基重氮甲烷反应,分别生成N-芳基氰基硫代甲酰苯胺铵盐,硫代氨基脲和2-(芳基氨基)-3,3-二苯基丙烯腈。他们还与芳基-,芳基双异氰酸酯和芳基异硫氰酸酯进行了几种亲电反应,生成单-和双-咪唑烷亚氨基硫酮和咪唑烷亚氨基二硫酮。用硫化氢,取代的邻苯二胺和硫代碳酰肼处理咪唑烷亚氨基硫酮,得到相应的硫代乙内酰脲,喹喔啉和咪唑三嗪衍生物。对几种合成产物进行了针对抗肿瘤,抗病毒,抗微生物和抗真菌菌株的体外生物学评估。大多数测试的化合物显示出显着的活性。

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