共查询到17条相似文献,搜索用时 90 毫秒
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以2-苄硫基-5-甲基-7-羟基-1,2,4-三唑并[1,5-a]嘧啶为原料,经醚化、肼解、成盐、关环和席夫碱反应合成了20个新型的含1,2,4-三唑-5-硫酮席夫碱的1,2,4-三唑并[1,5-a]嘧啶类化合物,通过IR,1H NMR,MS和元素分析对所合成的化合物进行了结构表征.初步生物活性测试结果表明,部分化合物表现出一定的抑菌或较好的抗烟草花叶病毒(TMV)活性.在500μg/mL浓度下,化合物6b,6f和6p对TMV的抑制率分别为41%,43%和40%. 相似文献
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以对称二氨基硫脲为原料,与冰醋酸反应生成5-甲基-4-氨基-1,2,4-三唑-3-硫酮(1);在弱酸性条件下,1与取代水杨醛反应生成席夫碱中间体5-甲基-4-(N-取代邻羟苯基)亚胺基-1,2,4-三唑-3-硫酮(2a~2c);最后在碱性条件下分别与N-取代苯基-2-氯乙酰胺发生烷基化反应生成15种未见报道的目标化合物3-(N-取代苯基-2-乙酰胺基)硫基-4-(N-取代邻羟苯基)亚胺基-5-甲基-1,2,4-三唑(3a~3o),其结构经IR,1H NMR,13C NMR确证.初步生物测试表明,质量分数为0.01%时,3a~3o对白色念珠菌的抑菌率均达90%以上,具有很强的抑菌活性;对金黄色葡萄球菌、大肠杆菌的抑菌率达80%以上,具有较强的抑菌活性. 相似文献
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在KOH/丙酮体系中, 以5-甲基-4-N-取代苯基亚胺/胺基-1,2,4-三唑-3-硫酮为原料, 与溴-α-D-四乙酰葡萄糖进行Kenigs-Knorr反应合成了10个新颖的化合物—5-甲基-4-N-取代苯基亚胺基/胺基-3-S-(2',3',4',6'-四-O-乙酰基-β-D-吡喃葡萄糖基)-1,2,4-三唑(2a~2e, 5a~5e); 并在二氯甲烷/甲醇/甲醇钠混合体系中水解脱除乙酰基, 得到10个新颖的化合物—5-甲基-4-N-取代苯基亚胺基-3-S-(β-D-吡喃葡萄糖基)-1,2,4-三唑(3a~3e)及5-甲基-4-N-取代苯基胺基-3-S-(β-D-吡喃葡萄糖基)-1,2,4-三唑(6a~6e). 化合物的结构均经核磁共振波谱(NMR)、 红外光谱(IR)和高分辨质谱(HRMS)分析确证. 生物活性测试结果表明, 目标化合物对大肠杆菌、 金黄色葡萄球菌、 枯草芽孢杆菌和白色念珠球菌普遍具有较好的抗菌活性. 化合物3d和3e对4种菌株的最小抑菌浓度相对较低, 表现出较强的广谱抗菌活性. 相似文献
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采用密度泛函理论(DFT)方法, 在B3LYP/6-31++G(d,p)水平上研究了4-亚芳基亚氨基-1,2,4-三唑-3(2H)-酮及其类似物的气相热分解反应. 从热力学性质、几何结构参数、自然电荷分布、温度效应等角度探讨不同取代基对标题物热分解反应的影响. 结果表明: R (R=H, CH2CH2CN)取代基对反应影响很小; 而苯环上Y (Y=MeO, Me, H, Cl和NO2)取代基对活化自由能(ΔG≠)、键长(ΔR≠)、键角(Δα≠)和自然电荷(Δq≠)变化的影响与Hammet常数(σ)呈现线性关系ΔP≠=ρσ+C (P=G, R, α和q, r>0.95). 给电子基团使得相应的活化自由能降低, 键长变短, 键角变大, 自然电荷增加; 吸电子反之. 相似文献
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4-氨基-5-烃基-2,4-二氢-3H-1,2,4-三唑-3-硫酮席夫碱的简便合成 总被引:9,自引:1,他引:9
近年来,人们发现标题类杂环席夫碱能发生很多新颖的反应,且其中许多具有强的生物活性[1~7].但其制备多以乙醇为反应介质,以酸或碱为催化剂,反应需经数小时,后处理也比较麻烦.本文报道了题示席夫碱的一种极为简便的合成方法,反应介质选用低级的脂肪酸(如冰醋... 相似文献
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本文报道了以(E)-1-(2-对甲苯磺酰胺基)-3-芳基丙-2-烯-1-酮(1)为底物与N-硫代丁二酰亚胺(2)通过亲电环化反应合成2-芳基-3-硫代-2,3-二氢喹啉-4(1H)-酮类化合物。以三氟化硼乙醚为催化剂(20 mol %),1,2-二氯乙烷为溶剂,反应温度为60 oC,可以60-92%的收率得到一系列2-芳基-3-硫代-4(1H)-喹啉酮衍生物,化合物3a-k均未见文献报道,其结构均经过1H NMR, 13C NMR以及高分辨质谱进行确定。 相似文献
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Highly efficient solid-phase synthesis of 4,5-disubstituted-1,2,4-triazole-3-thiones under mild conditions has been developed. 4,5-Disubstituted-1,2,4-triazole-3-thione derivatives were synthesized from resin-bound acylhydrazines in several steps, providing 76–89% overall yields and excellent purity. 相似文献
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S. M. Khripak M. V. Slivka R. V. Vilkov R. N. Usenko V. G. Lendel 《Chemistry of Heterocyclic Compounds》2007,43(6):781-785
The monohalogenation of 4-allyl-3-allylamino-1,2,4-triazole-5-thione has been studied. It was established that the action
of bromine and iodine on 4-allyl-3-allylamino-1,2,4-triazole-5-thione at low temperatures leads to selective closure of a
thiazoline ring.
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Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 6, pp. 922–926, June, 2007. 相似文献
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4-Amino-5-(4,6-diphenyl-2-pyrimidinyl)-3,4-dihydro-2H-1,2,4-trazole-3-thione is formed from the reaction of 4,6-diphenylpyrimidinecarboxylic
acid or its ethyl ester with thiocarbonyl hydrazide. Alkylation of the product leads to S-alkyl derivaties or 6-substituted
3-(4,6-diphenyl-2-pyriimidinyl)-7H-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazine. Acetylation of 4-amino-5-(4,6-diphenyl-2-pyrimidinyl)-3,4-dihydro-2H-1,2,4-triazole-3-thione
gave under different conditions monoacetyl-, diacetyl, and triacetyl derivatives at the amino group and the N(2) atom, whereas benzoylation gave a benzoyl group at the amino group and 3-(4,6-diphenyl-2-pyrimidinyl)-6-phenyl-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazole.
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Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 7, 1088–1094, July, 2007. 相似文献
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1INTRODUCTION Recently,compounds containing pyrazole,imida-zole,triazole(including benzotriazole),pyridine,tetrazole and indole have attracted much interest because they exhibit some fungicidal activity,plant-growth regulating activity and antibacterial acti-vity[1~10].Schiff bases also constitute a good type of biologically active substructure[11~14],and the sulfur-containing Schiff bases are particularly effective.Studies of pyrazole Schiff base-type fungicides andtriazole compounds c… 相似文献
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A novel compound 5-(p-tolyl)-4-[2-(2,4-dichlorophenoxy)acetamido]-1,2,4-tria zole- 3-thione 2a has been synthesized by the reaction of 5-(p-tolyl)-4-amino-1,2,4-triazole-3-thione 1 with 2-(2,4-dich/orophenoxy)acetyl ch/oride. Interestingly, the title compound 2 was obtained when 2a crystallizes from a mixed solution of petroleum ether and ethyl acetate, and it has been characterized by elemental analysis, IR, ^1H NMR spectra and single-crystal X-ray diffraction. The crystal belongs to the triclinic system, space group P1 with a = 9.780(5), b = 10.876(6), c = 11.615(6) /A, a = 104.822(7), β= 94.105(6), ), = 94.305(6)°, V= 1185.7(11)/A3, Z = 2,μ = 0.397 mm^-1, Mr= 497.39, Dx= 1.393 g/cm^3, F(000) = 516, S = 1.097, the final R = 0.0730 and wR = 0.2133 for 4111 unique reflections (Rint = 0.0525) with 3212 observed ones. The dihedral angles made by the triazole ring with the methyl- and chloro-substituted benzene rings are 43.5(7) and 50.2(9)°, respectively. Some intra- and intermolecular hydrogen bonds together with C-H…π interactions existing in the lattice stabilize the crystal structure. 相似文献
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COOEtCOCH3(CH3)2NNHNH2NNCH3OOEtNH2NH2NNCH3ONHNH2PhNCSNNCH3ONHNHCNHSOH-NNCH3NNHNPhS12345 1 INTRODUCTION A large number of 1,2,4-triazole derivatives have been synthesized in recent years[1~4]. Many of them are reported to exhibit broad spectrum biologi-… 相似文献