共查询到20条相似文献,搜索用时 15 毫秒
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为了寻找新型高效低毒的农药先导化合物,采用1-[(杂芳基)甲基]-5-甲基-1H-1,2,3-三唑基-4-甲酰氯与2-氨基-5-烷基-1,3,4-噻二唑的缩合反应,合成了8种未见文献报道的目标化合物,其结构经IR,1H NMR和元素分析确证,部分化合物还经MS的进一步证实.初步的生物活性测试结果表明,部分目标化合物在100 mg/L浓度下对双子叶植物(油菜)显示出中等的除草活性和一定程度的杀虫活性(250 mg/L). 相似文献
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超声辐射下合成1-[(未)取代苯酰基-3-[5-(1-苯基-3-甲基-5-氯吡唑-4-基)-1,3,4-噻二唑-2-基]-硫脲 总被引:2,自引:0,他引:2
1-苯基-3-甲基-5-氯吡唑-4-甲酸与氨基硫脲在三氯氧磷中反应得到2-氨基-5-(1-苯基-3-甲基-5-氯吡唑-4-基)-1,3,4-噻二唑(1), 然后分别采用超声辐射法和常规加热法与(未)取代苯甲酰基异硫氰酸酯(2)反应合成了一系列未见报到的1-[(未)取代苯酰基-3-[5-(1-苯基-3-甲基-5-氯吡唑-4-基)-1,3,4-噻二唑-2-基]-硫脲(3a~3j). 化合物的结构经元素分析, IR, 1H NMR确证. 相似文献
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Cyril Prknyi Hui Liang Yuan Bo H. E. Strmberg Ariella Evenzahav 《Journal of heterocyclic chemistry》1992,29(4):749-753
The synthesis of ten new substituted 1,3,4-thiadiazolyl-4(3H)-quinazolinones 8–11, 13, 17 , and 20–23 is reported. Compounds 8–11 were prepared by condensation of 5-fluoro-2-methyl-3,1-benzoxazin-4-one (3) and 5-substituted 2-amino-1,3,4-thiadiazoles 4–7. Compound 13 was obtained by condensation of 5-fluoro-2-methyl-3,1-benzoxazin-4-one (3) with DL-α-amino-?-caprolactam (12) . Compound 17 was synthesized by condensation of 6-bromo-2-methyl-3,1-benzoxazin-4-one (16) and 2-amino-5-t-butyl-1,3,4-thiadiazole (5) . Compounds 20–23 were obtained by condensation of 5-chloro-6,8-dibromo-2-methyl-3,1-benzoxazin-4-one (19) and 5-substituted 2-amino-1,3,4-thiadiazoles 4–7, respectively. The substituted 3,1-benzoxazin-4-ones 3, 16, and 19 were obtained in good yield by refluxing the appropriate anthranilic acid, 1,15 , and 18 with acetic anhydride (2) . 相似文献
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The title compound N-(2,6-difluorobenzoyl)-N'-[5-(4-trifluoromethylphenyl)-1,3,4-thiadiazol-2-yl]urea(C17H9F5N4O2S, Mr = 428.34) has been synthesized by the reaction of 2-amino-5-(4-trifluoromethylphenyl)-l,3,4-thiadiazole with 2,6-difluorobenzoyl isocyanate, and its
crystal structure was determined by single-crystal X-ray diffraction. The crystal belongs to monoclinic, space group P21/n with a = 10.7316(13), b = 10.5617(13), c = 16.037(2) (A), β =106.408(2)°, V= 1743.6(4) (A)3, Z = 4, Dc = 1.632 g/cm3, μ = 0.260 mm-1, F(000) = 864, the final R = 0.0599 and wR = 0.1420 for 3467 observed reflections with I > 2o(Ⅰ). The urea group, which adopts a planar configuration mediated by the intramolecular N-H…O hydrogen bond, is nearly coplanar with the thiadiazole and 4-trifluoromethylbenzene rings. The title compound was found to exhibit good fungicidal activity against Rhizoctonia solani and Botrytis cinerea. 相似文献
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为了寻找新型高效低毒的农药先导化合物, 采用1-[(杂芳基)甲基]-5-甲基-1H-1,2,3-三唑基-4-甲酰氯与2-氨基-5-烷基-1,3,4-噻二唑的缩合反应, 合成了8种未见文献报道的目标化合物, 其结构经IR, 1H NMR和元素分析确证, 部分化合物还经MS的进一步证实. 初步的生物活性测试结果表明, 部分目标化合物在100 mg/L浓度下对双子叶植物(油菜)显示出中等的除草活性和一定程度的杀虫活性(250 mg/L). 相似文献
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The title compound N-(2,6-difluorobenzoyl)-N'-[5-(4-trifluoromethylphenyl)-1,3,4-thiadiazol-2-yl]urea(C17H9F5N4O2S,Mr = 428.34) has been synthesized by the reaction of 2-amino-5-(4-trifluoromethylphenyl)-1,3,4-thiadiazole with 2,6-difluorobenzoyl isocyanate,and its crystal structure was determined by single-crystal X-ray diffraction.The crystal belongs to monoclinic,space group P21/n with a = 10.7316(13),b = 10.5617(13),c = 16.037(2) ,β = 106.408(2)°,V = 1743.6(4) 3,Z = 4,Dc = 1.632 g/cm3,μ = 0.260 mm-1,F(000) = 864,the final R = 0.0599 and wR = 0.1420 for 3467 observed reflections with I > 2σ(I).The urea group,which adopts a planar configuration mediated by the intramolecular N-H...O hydrogen bond,is nearly coplanar with the thiadiazole and 4-trifluoromethylbenzene rings.The title compound was found to exhibit good fungicidal activity against Rhizoctonia solani and Botrytis cinerea. 相似文献
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N-(5-三氟甲基-1,3,4-噻二唑-2-基)-N''-芳酰基脲的合成、晶体结构及生物活性 总被引:4,自引:3,他引:4
通过2-氨基-5-三氟甲基-1,3,4-噻二唑与芳酰基异氰酸酯反应,合成了10种新的芳酰基脲.它们的结构经元素分析、红外光谱、核磁共振氢谱进行了表征.并用X射线单晶衍射法测定了化合物2j的晶体结构,结果表明,该化合物晶体属三斜晶系,空间群为P-1,a=0.54191(15)nm,b=0.7766(2)nm,c=1.7161(5)nm,α=98.668(5)°,β=95.103(5)°,γ=101.070(5)°,V=0.6955(3)nm3,Z=2,Dc=1.653g/cm3,F(000)=352,μ=0.289mm-1.初步的生测试验结果表明一些目标化合物具有良好的植物生长调节活性. 相似文献
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N-[5-(1-邻(对)氯苯氧乙基)-1,3,4-噻二唑-2-基]-N'-芳酰基硫脲的合成与生物活性 总被引:4,自引:0,他引:4
为了寻找高活性的杂环农药,通过2-氨基-5-(1-邻氯苯氧乙基)-1,3,4-噻二唑和2-氨基-5-(1-对氯苯氧乙基)-1,3,4-噻二唑与芳酰基异硫氰酸酯反应,合成了26种新的芳酰基硫脲.采用核磁共振氢谱、红外光谱及元素分析确证了它们的结构.初步的生物活性测定试验表明,部分目标化合物表现出良好的植物生长调节活性,其中3c,3d,3e,4b和4c具有优良的生长素活性. 相似文献
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Guan-Ping Yu Wen-Zhao Bi Guo-Dong Si Ya-Xun Yang Haji Akber Aisa Liang-Zhong Xu 《Structural chemistry》2009,20(4):569-576
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. 相似文献
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以4-羟基香豆素为原料,经氯化、醚化和异硫氰酸化3步反应制得中间体——4-(4-异硫氰酸酯苯氧基)香豆素(3);3与取代芳香胺经加成反应合成了9个新型的1-(4-取代苯基)-3-[4-(4-氧香豆素基)苯基]硫脲衍生物(4a~4i),其结构经1H NMR,13C NMR,IR和MS(ESI)表征。采用浑浊度法测试了4的抑菌活性。结果表明:4a、4b、4e和4f抑制烟草青枯菌活性EC50值分别为112.02、121.39、88.72和86.90μg·mL~(-1),优于噻菌铜(130.25μg·mL~(-1));4a、4b、4e和4f抑制番茄青枯菌活性EC50值分别为107.89、110.69、82.43和82.48μg·mL~(-1),优于噻菌铜(123.94μg·mL~(-1))。 相似文献
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F. Firoozi K. Javidnia M. Kamali A. Fooladi A. Foroumadi A. Shafiee 《Journal of heterocyclic chemistry》1995,32(1):123-128
Starting from readily available ethyl-4-nitropyrrole-2-carboxylate ( 1 ), substituted 1-methyl-2-(1,3,4-thiadiazol-2-yl)-4-nitropyrroles and 1-methyl-2-(1,3,4-oxadiazol-2-yl)-4-nitropyrroles were prepared. The reaction of 1 with diazomethane gave ethyl 1-methyl-4-nitropyrrole-2-carboxylate ( 2 ). Reaction of compound 2 with hydrazine hydrate afforded the corresponding hydrazide 3 . The reaction of 3 with formic acid yielded 1-(1-methyl-4-nitropyrrole-2-carboxyl)-2-(formyl)hydrazine ( 7 ). Refluxing of the latter with phosphorus pentasulfide in xylene yielded compound 6 in 40% yield. Reaction of compound 7 with phosphorus pentoxide afforded compound 9 . Reaction of compound 3 with 1,1′-carboxyldiimidazole in the presence of triethylamine yielded 2-(1-methyl-4-nitro-2-pyrrolyl)-1,3,4-oxadiazoline-4(H)-5-one ( 11 ). Refluxing compound 3 with cyanogen bromide in methanol gave compound 12 . Compound 13 could be obtained through the reaction of compound 3 with carbon disulfide in basic medium. Alkylation of compound 13 afforded the correspanding alkylthio derivative 14 . Reaction of 1-methyl-4-nitropyrrole-2-carboxylic acid ( 15 ) with thiosemicarbazide and phosphorus oxychloride gave 2-amino-5-(1-methyl-4-nitro-2-pyrrolyl)-1,3,4-thiadiazole ( 16 ). Sandmeyer reaction of compound 16 yielded 2-chloro-5-(1-methyl-4-nitro-2-pyrrolyl)-1,3,4-thiadiazole ( 17 ). Refluxing of the latter with thiourea afforded 2-(1-methyl-4-nitro-2-pyrrolyl)-1,3,4-thiadiazoline-4(H)-5-thione ( 18 ). Alkylation of compound 18 gave the corresponding alkylthio derivative 19 . Oxidation of the latter with hydrogen peroxide in acetic acid yielded 2-(1-methyl-4-nitro-2-pyrrolyl)-5-methylsulfonyl-1,3,4-thiadiazole ( 20 ). 相似文献
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《中国化学快报》2016,(3)
This article demonstrates the synthesis, characterization and the study of in vitro antitubercular activities of twenty four new N-(4-(5-aryl-3-(5-methyl-1,3,4-oxadiazol-2-yl)-1H-pyrazol-1-yl)phenyl)-4-amide derivatives(8a–x). The antitubercular activity of the compounds against Mycobacterium tuberculosis H37Rv(MTB) revealed that 2-chloro-N-(4-(5-(4-chlorophenyl)-3-(5-methyl-1,3,4-oxadiazol-2-yl)-1H-pyrazol-1-yl)phenyl)benzamide(8n) is the most promising lead molecule with a MIC of1.56 mg/m L, while the corresponding unsubstituted benzamide derivative(8o) is the next most active molecule with a MIC of 3.13 mg/m L. Interestingly, the pyrazole intermediate 5b containing chlorophenyl and N-acylcarbohydrazide substituents also showed significant activity(MIC = 3.13 mg/m L). Further, the active molecules did not show toxicity against a normal NIH 3T3 cell line, signifying their suitability for further drug development. 相似文献