以3-芳基/烷基-4-氨基-5-巯基-1,2,4-三唑为原料,经过环化和糖化反应,设计合成了10个未见报道的化合物3-芳基/烷基-6-S-2',3',4',6'-四-O-乙酰基-β-D-吡喃葡萄糖基-1,2,4-三唑并[3,4-b]-1,3,4-噻二唑(3a^3j),其结构经...以3-芳基/烷基-4-氨基-5-巯基-1,2,4-三唑为原料,经过环化和糖化反应,设计合成了10个未见报道的化合物3-芳基/烷基-6-S-2',3',4',6'-四-O-乙酰基-β-D-吡喃葡萄糖基-1,2,4-三唑并[3,4-b]-1,3,4-噻二唑(3a^3j),其结构经核磁共振波谱、高分辨质谱和红外光谱确认.生物活性测试表明,所有化合物均对大肠杆菌、金黄色葡萄球菌、枯草芽孢杆菌和白色念株菌表现出一定的抗菌活性,其中化合物3c对4种测试菌株的最小抑菌浓度(MIC)最低,且接近于氟康唑的参照数据,具有较强的抗菌活性.利用Auto Dock 4.0程序研究了目标化合物3a^3j与大肠杆菌FabⅠ受体蛋白分子的相互作用和结合自由能变化规律.展开更多
In recent years, fused heterocycles have been reported to possess important properties in synthesis and pharmacology. Especially, s-triazolo, 3,4-thiadiazole derivatives have been attracting much attention for chemist...In recent years, fused heterocycles have been reported to possess important properties in synthesis and pharmacology. Especially, s-triazolo, 3,4-thiadiazole derivatives have been attracting much attention for chemists and pharmacologists because they show broad spectra of biological activities, such as antifungal, antibacterial, hy-展开更多
6/3-（4-Chlorophenyl）-s-triazolo[3, 4-b][1, 3, 4]thiadiazoles （2,a-e） and （Sa-e） were synthesized respectively by intermolecular cyclization of 5-aryl / 4-chlorophenyl-4-amino-3- mercapto-1, 2, 4-triazoles （la-e...6/3-（4-Chlorophenyl）-s-triazolo[3, 4-b][1, 3, 4]thiadiazoles （2,a-e） and （Sa-e） were synthesized respectively by intermolecular cyclization of 5-aryl / 4-chlorophenyl-4-amino-3- mercapto-1, 2, 4-triazoles （la-e） and （4） with 4-chlorobenzoic acid / aryl acids, which were condensed with piperazine under phase transfer catalyst TBAB to yield the corresponding free bases of monopiperazine derivatives and followed to form water-soluble salts （3a-e） and （6a-e） with hydrochloric acid in good yields. The in vitro biological results showed that piperazine group conjugated with the above fused heterocycles played an important role in antibacterial activity. The structures of novel compounds were confirmed by IR, ＇H NMR, MS and elemental analysis.展开更多
The rearrangement reaction of 2-benzothiazolylthioacetyl hydrazide 1 with potassium hydroxide and carbon disulfide in ethanol to produce s-triazolo[3, 4-b]benzothiazole-3-thiol 3 was described. 3 also can be obtained...The rearrangement reaction of 2-benzothiazolylthioacetyl hydrazide 1 with potassium hydroxide and carbon disulfide in ethanol to produce s-triazolo[3, 4-b]benzothiazole-3-thiol 3 was described. 3 also can be obtained from 2-benzothiazolylhydazine 2 and the two methods for getting 3 were compared. Mannich reaction of compounds 3 was reported too.展开更多
A novel rearrangement reaction about 2-benzothiazolyl-thioacetyl hydrazide(1) to produce s-triazolo[3, 4-b] benzoth-iazol-3-thiol (3) in the presence of KOH and CS_2 wasdescribed. Other way to synthesize 3 from 2-benz...A novel rearrangement reaction about 2-benzothiazolyl-thioacetyl hydrazide(1) to produce s-triazolo[3, 4-b] benzoth-iazol-3-thiol (3) in the presence of KOH and CS_2 wasdescribed. Other way to synthesize 3 from 2-benzothiazolyl-hydrazine (2) under the same conditionwas compared and the Mannich reaction of compound 3 was reported too. Their structures wereestablished by elemental analyses, IR, ~1H NMR and MS spectra.展开更多
In this paper , 10 novel 6-aryl-3-(5'-phenyl-2H-tetrazole-2'-methylene)-S-triazolo[3, 4-b]-1,3,4-thiadiazoles have been synthesized by the condensation of 3-(5'-phenyl-2H-tetrazole-2'-methylene)-4-amin...In this paper , 10 novel 6-aryl-3-(5'-phenyl-2H-tetrazole-2'-methylene)-S-triazolo[3, 4-b]-1,3,4-thiadiazoles have been synthesized by the condensation of 3-(5'-phenyl-2H-tetrazole-2'-methylene)-4-amino-5-mercapto-1,2,4-triazole with various aromatic carboxylic acids in the presence of phosphorus oxychloride. The structure of these compounds was determined by elemental analysis , UV, IR, 1H NMR and MS. Their spectral properties were also discussed.展开更多
文摘以3-芳基/烷基-4-氨基-5-巯基-1,2,4-三唑为原料,经过环化和糖化反应,设计合成了10个未见报道的化合物3-芳基/烷基-6-S-2',3',4',6'-四-O-乙酰基-β-D-吡喃葡萄糖基-1,2,4-三唑并[3,4-b]-1,3,4-噻二唑(3a^3j),其结构经核磁共振波谱、高分辨质谱和红外光谱确认.生物活性测试表明,所有化合物均对大肠杆菌、金黄色葡萄球菌、枯草芽孢杆菌和白色念株菌表现出一定的抗菌活性,其中化合物3c对4种测试菌株的最小抑菌浓度(MIC)最低,且接近于氟康唑的参照数据,具有较强的抗菌活性.利用Auto Dock 4.0程序研究了目标化合物3a^3j与大肠杆菌FabⅠ受体蛋白分子的相互作用和结合自由能变化规律.
文摘In recent years, fused heterocycles have been reported to possess important properties in synthesis and pharmacology. Especially, s-triazolo, 3,4-thiadiazole derivatives have been attracting much attention for chemists and pharmacologists because they show broad spectra of biological activities, such as antifungal, antibacterial, hy-
基金This project was supported by the State Basic Research and Development Project(No.G1998051112).
文摘6/3-（4-Chlorophenyl）-s-triazolo[3, 4-b][1, 3, 4]thiadiazoles （2,a-e） and （Sa-e） were synthesized respectively by intermolecular cyclization of 5-aryl / 4-chlorophenyl-4-amino-3- mercapto-1, 2, 4-triazoles （la-e） and （4） with 4-chlorobenzoic acid / aryl acids, which were condensed with piperazine under phase transfer catalyst TBAB to yield the corresponding free bases of monopiperazine derivatives and followed to form water-soluble salts （3a-e） and （6a-e） with hydrochloric acid in good yields. The in vitro biological results showed that piperazine group conjugated with the above fused heterocycles played an important role in antibacterial activity. The structures of novel compounds were confirmed by IR, ＇H NMR, MS and elemental analysis.
基金supported by the National Natural Science Foundation of China(QT group).
文摘The rearrangement reaction of 2-benzothiazolylthioacetyl hydrazide 1 with potassium hydroxide and carbon disulfide in ethanol to produce s-triazolo[3, 4-b]benzothiazole-3-thiol 3 was described. 3 also can be obtained from 2-benzothiazolylhydazine 2 and the two methods for getting 3 were compared. Mannich reaction of compounds 3 was reported too.
文摘A novel rearrangement reaction about 2-benzothiazolyl-thioacetyl hydrazide(1) to produce s-triazolo[3, 4-b] benzoth-iazol-3-thiol (3) in the presence of KOH and CS_2 wasdescribed. Other way to synthesize 3 from 2-benzothiazolyl-hydrazine (2) under the same conditionwas compared and the Mannich reaction of compound 3 was reported too. Their structures wereestablished by elemental analyses, IR, ~1H NMR and MS spectra.
基金Project supported by the National Natural Science Foundation of China.
文摘In this paper , 10 novel 6-aryl-3-(5'-phenyl-2H-tetrazole-2'-methylene)-S-triazolo[3, 4-b]-1,3,4-thiadiazoles have been synthesized by the condensation of 3-(5'-phenyl-2H-tetrazole-2'-methylene)-4-amino-5-mercapto-1,2,4-triazole with various aromatic carboxylic acids in the presence of phosphorus oxychloride. The structure of these compounds was determined by elemental analysis , UV, IR, 1H NMR and MS. Their spectral properties were also discussed.
