酰氨基硫脲及其相关杂环衍生物的研究II.1-[5-(α-萘)-2H-四唑-2-乙酰[-4-苯基氨基硫脲及其相关环衍生物的合成

本文合成了1-[5-(α-萘)-2-H-四唑2-乙酰]-4-苯基氨基硫脲5,以及由5衍生的环化产物3-[5-(α-萘)-2H-四唑2-甲撑]-4-苯基-1,2,4-三咪啉-5-硫酮6,2-苯胺基-5-[5-(α-萘)-2H-四唑-2-甲撑]-1,3,4-噻二唑7及2-苯胺基-5-[5-(α-萘)-2H-四唑-2-甲撑]-1,3,4-二唑8.它们的结构均通过元素分析,红外光谱,核磁共振及质谱鉴定.其药理实验正在进行中.初步实验表明,5及6对小麦生长有较强的促进作用.     

酰氨基硫脲及其相关的杂环衍生物的研究——Ⅴ.1-(β-吗啉丙酰基)-4-芳基氨基硫脲及其相关杂环衍生物的合成

前文已报道某些1-酰基-4-取代氨基硫脲及其相关杂环衍生物具有广泛的生理活性,如抗结核,抗真菌,解痉挛及促进植物生长等功效。为进一步观察酰氨基硫脲及其杂环衍生物的有关活性,我们以β-吗啉丙酰肼(1)同一系列芳基异硫氰酸酯(2)进行反应,试图制得各种1-(β-吗啉丙酰基)-4-取代芳基氨基(3),并研究3在酸或碱性条件下的环化     

酰氨基硫脲及其相关杂环衍生物的研究——Ⅻ.1-(α-苯基氰乙酰胺基)-3-芳酰基硫脲及3-(α-苯基氰甲基)-4-芳酰基-1,2,4-三唑-5-硫酚衍生物的合成

前文报道氰乙酰肼同芳基或芳酰基异硫氰酸酯缩合制得的一些新的酰胺基硫脲及其相关杂环衍生物,并观察到这些衍生物大多具有较强的生物活性。进一步研究发现,除氰乙酰肼以外,5-甲基异恶唑-3-甲酰肼,β-吗啉丙酰肼,异烟酰肼等同芳基异硫氰酸酯的加成产物也有促进小麦、蕃茄、黄瓜等农作     

酰氨基硫脲及其相关杂环衍生物的研究III.1-(5-甲基异唑-3-甲酰基)-4-芳基氨基硫脲及其相关杂环衍生物

Eight 1-(5-methylisoxazol-3-ylcarbonyl)-4-substituted thiosemicarbazides (I), eight 3-(5-methylisoxazol-3-yl)-4-substituted-1,2,4-triazoline-5-thiones (II), seven 2-arylamino-5-(5-methylisoxazol-3-yl)-1,3,4-thiadiazoles, and five 2-arylamino-5-(5-methylisoxazol-3-yl)-1,3,4-oxadiazoles were prepared from isoxazole III and aryl isocyanates. The derivatives I and II showed antitubercular activity and promoted the growth of plumule of wheat in preliminary experiments     

酰氨基硫脲及其相关杂环衍生物的研究 XII: 1-(α-苯基氰乙酰胺基)-3-芳酰基硫脲及3-(α-苯基氰甲基)-4-芳酰基-1,2,4-三唑-5-硫酚衍生物的合成

报导了α-苯基氰乙酰肼同异硫氰酸酯反应, 制得一系列1-(α-苯基氰乙酰胺基)-3-芳酰基硫脲的新衍生物, 用二分子酰胺基硫脲衍生物与一克分子NaH进行催化反应可环化成1,2,4-三唑衍生物.     

酰氨基硫脲及其相关杂环衍生物的研究(ⅩⅧ)——5-[5-(3-吡啶)-四唑-2-亚甲基]-2-芳氨基-1,3,4-噻二唑的合成及其抗菌活性

四唑和噻二唑类衍生物具有广泛的生物活性,如抗真菌、抗霉菌、抗肿瘤、抗结核菌,以及促进植物生长等活性,1,4-二取代酰氨基硫脲是合成此类物质的重要原料,为了深入研究同一分子中聚结各种杂环化合物的合成及生物活性。     

5-[5-(3-吡啶)-2H-四唑亚甲基]-2-芳酰氨基-1,3,4-噻二唑的合成

正如前文报道,l,3,4—噻二唑类杂环之所以有除草,植物生长调节,驱虫以及消炎等多种生物活性,无疑起因于噻唑母核。尽管母核上取代基不起主导作用,但它作为辅助基,在改善分子溶解性以及药效方面所产生的影响是不能忽略的。因而深入研究各种生物活性基团导入噻二唑环母核以制得多结构单元聚集于同一分子中的噻二唑新衍生物,对于开发多功能新药具有一定的理论意义和实际价值。     

酰氨基硫脲及其相关杂环衍生物的研究(ⅩⅦ)——1-芳酰基-4-[4′-(2,2,6,6-四甲基哌啶)-1-氧]-氨基硫脲的合成

本文报道21种新的1-芳酰基-4[4′-2,2,6,6-四甲基哌啶)-1-氧]-氨基硫脲化合物(5_(a-u)的合成,利用IR、MS和ESR谱确认了产品结构,讨论了IR、MS、ESR谱的性质,初步观察了5_(a-u)对L_(7712)白血病细胞的抑制作用。     

STUDIES ON THE SYNTHESIS OF THIOLS AND THEIR S-SUBSTITUTED DERIVATIVES

Abstract

Aromatic thiols belong to a group of not yet sufficiently explored compounds. The presence of an active hydrogen atom makes it possible to conduct various chemical conversions and to obtain new S-substituted derivatives.     

杂环息夫碱化合物及其过渡金属配合物的合成与表征

本文合成了一种新的双齿(N,O)杂环息夫碱2-(2′-羟基)苯甲亚胺-5-(4′-硝基)偶氮苯吡啶(HL)与过渡金属的六种新配合物ML_2及M′L_3 [M=Mn(Ⅱ)、Co(Ⅱ)、Ni(Ⅱ)、Cu(Ⅱ)、Pd(Ⅱ);M′=Fe(Ⅲ)].采用元素分析、摩尔电导、红外光谱、紫外—可见光谱、磁化率以及热分析等研究了配合物的组成和性质.     

含硒杂环化合物的合成和对超氧阴离子作用的ESR研究

引言硒作为人体必需的微量元素,其主要生化作用与谷胱甘肽过氧化物酶密切相关.在体内,该酶可以催化许多过氧化物的分解,并且与谷胱甘肽一起组成一个强有力的细胞防御体系,发挥其抗氧化作用.近几年来,人们发现了一种小分子有机硒化物2-苯基-1,2-苯并异硒唑酮-3(简称Ebselen)具有类似谷胱甘肽过氧化物酶的活性.它能有效地抑制活性氧自由基的产生而引起的细胞损伤,具有良好的抗炎活性,且毒性极低(大鼠LD_(50)>6180mg/os).因而,普遍认为Ebselen及其类似物是一类具有广谱抗炎活性的潜在药物,在医药领域具有广阔的应用前景.     

含氮杂环三烃基锡衍生物的合成及其生物活性

本文合成了14个含氮杂环三烃基锡衍生物,红外光谱,核磁共振谱和质谱的研究表明三烃基锡-1,2,4-三氮唑为以氮原子作桥联的五配位聚合结构化合物,化合物的生物活性和生物选择性主要取决于锡原子上的三烃基。     

氨基硫脲及其相关化合物的化学

本文综述了氨基硫脲及其相关化合的合成、波谱和化学性质以及在药物、工业、农业等方面的应用。     

MASS SPECTRAL FRAGMENTATION STUDIES ON THIOPHENOTROPONE AND THIOPHENOTROPILIDENE DERIVATIVES AND THEIR METAL TRICARBONYL COMPLEXS

Abstract

The mass spectral fragmentation of thiophenotropone, thiophenotropilidene derivatives and their iron and chromium tricarbonyl complexes are fully reported and discussed. The fragmentation patterns of the complexes are characterised by successive loss of three carbonyl groups. In general, the resulting ions after elimination of the metal behave in the same manner as the organic ligand. The iron complexes behave differently from their corresponding chromium complexes. The thiopheno[b]tropilidene iron tricarbonyl complex and its isomer thiopheno[c]tropilidene iron tricarbonyl complex could not be differentiated by mass spectrometry, such differentiation was achieved by proton magnetic resonance.     

STUDIES ON CHROMONES AND XANTHONE DERIVATIVES

Abstract

2-Methyl-6-phenyl chromone la and a variety of its derivatives were synthesized. The reactivity of In and other chromones with aromatic aldehydes, hydrazine hydrate, hydrazine derivatives. Hydroxylamine hydrochloride, different primary amines and Grignard reagents was investigated. The I.R. and H¹NMR spectra of the products are discussed.     

STUDIES IN THE HETEROCYCLIC SERIES. XIV. THE CHEMISTRY AND BIOLOGICAL ACTIVITY OF NEW AZA- AND THIA-PHENOTHIAZINES,AND RELATED DIBENZOTHIAZEPINES

Abstract

Owing to increasing demand for phenothiazine compounds both in medicine and industry, novel rings in these series have been prepared and evaluated. The benzene rings have been replaced with pyrrole, pyrazole, pyridine, pyridazine, pyrimidine, pyrazine, thiazine and triazine rings or their combinations leading to twelve new polyaza- and thia-phenothiazines. Expansion of the central thiazine ring in these systems has also been carried out. This article therefore provides a survey of the chemistry and applications of new polyaza- and thia-phenothiazine systems and their related thiazepines and thiazocines.