某些含三唑取代的苯甲酸苯甲酰甲酯衍生物的合成

以三乙胺为缚酸剂，通过苯甲酸同ω－（１Ｈ－１，２，４－三唑－１－基）－ω－溴化苯乙酮反应，合成了六种含三唑取代的苯甲酸甲酰甲酯类化合物，具有较高收率。     

1－芳氧乙酰氧基－1－（1H－1，2，4－三唑－1－基）－3，3－二甲基－2－丁酮衍生物的研究

以三乙胺为缚酸剂，用芳氧乙酸同ω－溴代－ω－（１Ｈ－１，２，４－三唑－１－基）频哪酮反应，合成了一系列三唑类新化合物，探讨了化合物的合成方法。通过ＩＲ￣１ＨＮＭＲ、ＭＳ分析及元素分析确定了化合物的结构，生物活性测定结果表明，部分化合物具有良好的除草活性，同时表现出一定程度的植物生长调节活性及杀菌活性．     

ω－芳氧乙酰氧基－ω－（1H－1，2，4－三唑－1－基）苯乙酮衍生物的研究

报道了１５种含三唑取代的芳氧乙酸苯甲谈甲酯类新化合物；产物的结构经ＩＲ、１ＨＮＭＲ、ＭＳ及元素分析证实。生物活性测定结果表明：部分化合物表现出良好的除草或杀菌及植物生长调节活性。     

α－羰基－α－（1H－1，2，4－三唑－1－基）乙烯基芳基酮衍生物的合成及生物活性研究

α－（１Ｈ－１，２，４－三唑－１－基）取代苯乙酮与异硫氰酸苯酯在强碱条件下经缩合、卤化后得到含三唑的烯酮氮硫缩醛化合物１．该化合物与各种卤代物反应，形成了包括五元、六元杂环的缩合产物。部分结构具有一定的植物生长调节活性。     

1－（取代异噁唑基）－1，2，4．三唑和1－（取代嘧啶基）－1，2，4－三唑的合成及生物活性

合成了１５个新的１－（取代异噁唑基）－１，２，４－三唑和１－（取代嘧啶基）－１，２，４－三唑化合物，经元素分析、ＩＲ、１ＨＮＭＲ和ＭＳ证实其结构，并对其代表化合物进行了抑菌及植物生长调节活性的初步观察     

1－（取代吡唑－4－基）－1，2，4－三唑的合成及生物活性研究

合成了２３个新的１－（取代吡唑－４－基）１，２，４－三唑化合物，经ＥＡ、ＩＲ、~１ＨＮＭＲ和ＭＳ确定其组成和结构，并对其进行了抑菌及生长调节活性的初步观察。     

3－芳基－1（2H，4H）－吖啶酮衍生物的合成及其镇痛作用

３－芳基－１（２Ｈ，４Ｈ）－吖啶酮衍生物的合成及其镇痛作用韩光范，魏永慧，尹荣王进军姜贵吉（吉林医学院检验系吉林１３２００１）（吉林化工学院精细化工系吉林）（延边大学化学系延吉）关键词吖啶酮衍生物，合成，镇痛作用吖啶及吖啶酮类化合物具有抗疟、抗菌、抗...     

酰氨基硫脲及相关杂环衍生物研究（XXV）──1－［5′－氨基－1′－（4″－氯苯基）－1′，2′，3′－三唑－4′－甲酰基］－4－芳基氨基硫脲的合成和波谱研究

通过５－氨基－１－（４′－氯苯基）－４－甲酰肼基－１，２，３－三唑与芳基异硫氰酸酯的反应，合成了１３种新的１－［５′－氨基－１′－４″－氯苯基）－１′，２′，３′－三唑－４′－甲酰基］－４－芳基氨基硫脲类化合物３ａ－１，经元素分析、ＩＲ、１ＨＮＭＲ以及ＭＳ确证其结构。     

有机锡2-[(1,2,4-三唑-1-基)甲基硫代]苯甲酸酯的合成与生物活性

通过硫代水杨酸与(1-氯甲基)-1,2,4-三唑盐酸盐在碱性条件下的反应, 合成了2-[(1,2,4-三唑-1-基)甲基硫代]苯甲酸. 利用该酸与(R₃Sn)₂O(R=Et, n-Bu, Ph), Cy₃SnOH(Cy为环己基)或Et₂SnO反应, 得到了5个有机锡羧酸酯. 用X射线单晶衍射测定了三正丁基锡2-[(1,2,4-三唑-1-基)甲基硫代]苯甲酸酯的晶体结构. 在该化合物中, 锡为五配位的三角双锥结构. 该化合物通过三唑四位氮原子与锡配位, 形成一维链状配位高分子. 初步的生物活性测试结果表明, 所有的有机锡化合物都表现出了明显的抗真菌活性.     

Synthesis and QSAR studies on 1-[(5-substituted-1,3,4-thiadiazol-2-yl)methyl]-1H-1,2,4-triazole as antifungal agents

A series of 1-[(1,3,4-thiadiazol-2-yl)methyl]-1H-1,2,4-triazole derivatives were prepared and evaluated for their antifungal activities. The chemical structures of these compounds were determined by means of elemental analyses, ¹H NMR, and X-ray crystallography. Quantitative structure–activity relationship (QSAR) studies were performed on these compounds using physicochemical parameters as independent parameters and antifungal activity as a dependent parameter, where antifungal activity correlated best (r > 0.9) with hydrophobic parameters (π) and indicator (H). Moreover, the results are interpreted on the basis of a multiple regression model. The model has been internally and externally validated. Furthermore, the domain of applicability which indicates the area of reliable predictions is defined.     

1—芳氧乙酰氧基—1—（1H—1,2,4—三唑—1—基）—3,3—二甲基—2—丁酮衍生物…

以三乙胺为缚酸剂，用芳氧乙酸同ω－溴化－ω－（１Ｈ－１，２，４－三唑－１－基）频哪酮反应，合成了一系列三唑类新化合物，探讨了化合物的合成方法。通过ＩＲ、＾１Ｈ ＮＭＲ、ＭＳ分析及元素分析确定了化合物的结构。生物活性测定结果表明，部分化合物具有良好的除草活性，同时表现出一定程度的植物生长调节活性及杀菌活性。     

3-Aryl-5-[(aryloxy)methyl]-3-[(1H-1,2,4-triazol-1-yl)methyl]-2-methylisoxazolidine derivatives. Synthesis and antifungal activity

The synthesis and antifungal activity of a novel series of 3-aryl-5-[(aryloxy)methyl]-3-[(1H-1,2,4-triazol-1-yl)-methyl]-2-methylisoxazolidines are described. The in vitro activity was evaluated in solid agar cultures against a variety of dermatophytes and yeast fungi, while in vivo activity was measured in an immune-compromised mouse model of systemic candidiasis. The activity of the title series was compared to that of ketoconazole and one derivative, the cis-3-(4-chlorophenyl)-5-(4-chlorophenyloxy)methyl analogue 5f was found to possess a similar potency in the in vivo assay. Structure-activity relationship correlations are also discussed.     

Synthesis and Crystal Structure of 5-[（1H-1,2,4-Triazol-1- yl）methyl]-4-（2,3-dimethoxybenzylideneamino）-2- 2H-1,2,4-triazole-3（4H）-thione Monohydrate

1 INTRODUCTION Heterocyclic compounds bearing the 1,2,4-tri- azole moiety have attracted considerable attention over the past few decades since they exhibit some fungicidal activities against Puccinia recondite and applications in the field of root-growth regu- lation[1~3]. Meanwhile, 4-amino-5-mercapto-1,2, 4-triazole moiety has great versatility in fusing tovarious ring systems and possesses a broad spec- trum of biological activities[4, 5]. In our con- tinuous work directed towards the…     

Synthesis and properties of 1-[(adamantan-1-yl)methyl]-3-pyrazolyl ureas

Chemistry of Heterocyclic Compounds - A series of 1,3-disubstituted ureas containing 1,3,5-trisubstituted pyrazole and (adamantan-1-yl)methyl fragments were synthesized in the reaction of...     

Synthesis of 5-[(Thiophen-3-yl)amino]-1,2,4-triazines

Russian Journal of Organic Chemistry - Methyl 3-(3,6-diaryl-1,2,4-triazin-5-ylamino)thiophen-2-carboxylates were synthesized in 70–75% yield by solvent-free reaction of methyl...