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合成了18个新型含苯并噁/噻唑啉酮结构的2,6-二取代咪唑[2,1-b][1,3,4]噻二唑衍生物5a~5i', 即2-[(2-苯并噁/噻唑啉酮-3-基)甲基]-6-芳基-咪唑[2,1-b][1,3,4]噻二唑. 利用红外光谱、 核磁共振和元素分析对化合物的结构进行了表征. β2-肾上腺素受体(β2-AR)拮抗剂钙流筛选结果表明, 部分目标化合物对β2-AR具有明显的拮抗作用, 其中化合物5c'的拮抗效果最高, 为70%. 这些化合物可作为潜在的β2-AR拮抗剂. 相似文献
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以2-氨基-5-取代苯氧甲基-1,3,4-噻二唑(1)为起始原料, 合成了中间体2-氯乙酰氨基-5-取代苯氧甲基-1,3,4-噻二唑)-2-乙酰亚胺(2)和2-(5-取代苯氧甲基-1,3,4-噻二唑-2-亚胺基)-4-噻唑啉酮(3), 化合物3进一步与取代苯甲醛发生类Knoevenagle缩合反应, 得到了一系列2-(5-取代苯氧甲基-1,3,4-噻二唑-2-亚胺基)-5-(取代苯基亚甲基)-4-噻唑啉酮类化合物4a~4p. 目标化合物4a~4p的结构经IR, 1H NMR和元素分析确证. 相似文献
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根据活性基团拼合原理, 用2-氯硒基苯甲酰氯和2-氨基-5取代-1,3,4-噻二唑缩合合成了10个新的2-(2-取代- 1,3,4-噻二唑-5-基)-苯并异硒唑-3(2H)-酮衍生物(6), 并通过IR, 1H NMR, ESI-MS和元素分析对其结构进行了确认, 采用CCK-8法测试了化合物抑制肿瘤细胞增殖活性. 结果表明, 化合物6h对人体肺癌细胞A-549, 化合物6a, 6b, 6d, 6e, 6f, 6g, 6h, 6j对人体乳腺癌细胞MCF-7, 化合物6a, 6b, 6d, 6e, 6f, 6g对人体肝癌细胞SSMC-7721抑制活性均强于阳性对照药依布硒啉, 且表现出一定的选择性, 具有进一步研究的潜在价值. 相似文献
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2′-芳基-3-(1,4,5,6-四氢-6-哒嗪酮-3-羰基)氨基硫脲及其环化产物的合成 总被引:4,自引:1,他引:4
以α-酮戊二酸为起始原料,合成了1,4,5,6-四氢-6-哒嗪酮-3-甲酰肼(2),然后将2与异硫氰酸芳基酯反应得到相应的芳基氨基硫脲衍生物3a~3f.用硫酸、醋酸汞或氢氧化钠分别将芳基氨基硫脲环化得到一系列新的1,3,4-噻二唑、1,3,4-噁二唑和1,2,4-三唑的衍生物.化合物的结构经元素分析,IR,1H NMR和MS谱得以证实. 相似文献
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酰氨基硫脲及其相关杂环衍生物的研究(Ⅴ)——1-(吡啶-4′-甲酰基)-4-芳基氨基硫脲及其相应的氮、硫、氧五员杂环化合物的合成 总被引:13,自引:4,他引:9
本文合成了一些新的1-(吡啶-4'-甲酰基)-4-芳基氨基硫脲(Ⅰ)、1,2,4-三唑啉-5-硫酮(Ⅱ)、1,3,4-噻二唑(Ⅲ)和1,3,4-嗯二唑(Ⅳ)衍生物。实验表明化合物(Ⅰ)在低浓度时对小麦、黄瓜等农作物的生长有显著的促进作用。 相似文献
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3-杂环基硫取代-1,3,4,5-四氢-2-氧代-苯并氮杂衍生物的合成 总被引:1,自引:0,他引:1
以芳酰肼为原料,合成了一系列3-巯基-5-芳基-1,2,4-三唑、2-巯基-5-芳基-1,3,4-噁二唑和2-巯基-5-芳基-1,3,4-噻二唑,并通过硫原子对3-溴-2-氧代-苯并氮杂3-位上的亲核取代反应将杂环化合物引入了苯并氮杂的结构当中,合成了32个新的苯并氮杂杂环衍生物.为提高其在有机溶剂中的溶解性,在苯并氮杂的N原子上引入乙酸乙酯和乙酸叔丁酯基取代基,合成了36个新衍生物.所有化合物经质谱、核磁共振谱及元素分析确证了结构并初步测定了抗菌活性. 相似文献
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以芳酰肼为原料, 合成了一系列3-巯基-5-芳基-1,2,4-三唑、2-巯基-5-芳基-1,3,4-噁二唑和2-巯基-5-芳 基-1,3,4-噻二唑, 并通过硫原子对3-溴-2-氧代-苯并氮杂3-位上的亲核取代反应将杂环化合物引入了苯并氮杂的结构当中, 合成了32个新的苯并氮杂杂环衍生物. 为提高其在有机溶剂中的溶解性, 在苯并氮杂的N原子上引入乙酸乙酯和乙酸叔丁酯基取代基, 合成了36个新衍生物. 所有化合物经质谱、核磁共振谱及元素分析确证了结构并初步测定了抗菌活性. 相似文献
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10.
《化学研究与应用》2015,(7)
合成了四种噻二唑衍生物:2,5-二苯基-1,3,4-噻二唑(DPTD),2,5-二(2-羟基苯)-1,3,4-噻二唑(2-DHPTD),2,5-二(3-羟基苯)-1,3,4-噻二唑(3-DHPTD)和2,5-二(4-羟基苯)-1,3,4-噻二唑(4-DHPTD)。采用Tafel极化测试、电化学阻抗谱(EIS)和扫描电子显微镜(SEM)研究了噻二唑衍生物在50 mg·L-1硫-乙醇体系中对银的缓蚀作用。实验结果表明:添加缓蚀剂后,银片腐蚀得到抑制,且缓蚀效率大小顺序为:[DPDT][2-DHPDT][3-DHPDT][4-DHPDT]。通过量子化学计算和分子动力学模拟进一步研究了四种噻二唑衍生物的缓蚀机理,理论计算结果与实验结果一致。 相似文献
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New coumarin derivatives, namely 7-[(5-amino-1,3,4-thiadiazol-2-yl)methoxy]-2H-chromen-2-one, 5-[(2-oxo-2H-chromen-7-yloxy)methyl]-1,3,4-thiadiazol-2(3H)-one, 2-[2-(2-oxo-2H-chromen-7-yloxy)acetyl]-N-phenylhydrazinecarbothioamide, 7-[(5-(phenylamino)-1,3,4-thiadiazol-2-yl)methoxy]-2H-chromen-2-one and 7-[(5-mercapto-4-phenyl-4H-1,2,4-triazol-3-yl)methoxy]-2H-chromen-2-one were prepared starting from the natural compound umbelliferone. The newly synthesized compounds were characterized by elemental analysis and spectral studies (IR, 1H-NMR and 13C-NMR). 相似文献
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2‐Alkyl‐, 2‐aryl‐, and 2‐halo‐substituted derivatives of 7‐methyl‐6‐fluoro‐1,3,4‐thiadiazolo[3,2‐a]pyrimidin‐6‐one ( 3 ) were prepared by reaction of 2‐substituted 5‐amino‐1,3,4‐thiadiazoles ( 1 ) and ethyl 2‐fluoroacetoacetate ( 2 ) in polyphosphoric acid. A convenient procedure was developed for the synthesis of new 2‐amino derivatives of 2‐R‐7‐methyl‐6‐fluoro‐1,3,4‐thiadiazolo[3,2‐a]pyrimidin‐6‐one ( 5 ). J. Heterocyclic Chem., (2011). 相似文献
13.
K. L. Borisova G. I. Mel��man V. A. Denisenko V. P. Glazunov V. F. Anufriev 《Russian Chemical Bulletin》2012,61(3):616-622
6(7)-(Di)alkyl- and 6(7)-(di)alkoxy derivatives of 2,3-dihydroxynaphthazarin were converted to 5,8-dihydroxyisoquinoline-1,3,4(2H)-trione derivatives under amination reaction conditions. 相似文献
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Chen Z Xu W Liu K Yang S Fan H Bhadury PS Hu DY Zhang Y 《Molecules (Basel, Switzerland)》2010,15(12):9046-9056
Starting from 4-chlorobenzoic acid, 10 new 5-(4-chlorophenyl)-N-substituted-N-1,3,4-thiadiazole-2-sulfonamide derivatives were synthesized in six-steps. Esterification of 4-chlorobenzoic acid with methanol and subsequent hydrazination, salt formation and cyclization afforded 5-(4-chlorophen-yl)-1,3,4-thiadiazole-2-thiol (5). Conversion of this intermediate into sulfonyl chloride 6, followed by nucleophilic attack of the amines gave the title sulfonamides 7a-7j whose structures were confirmed by NMR, IR and elemental analysis. The bioassay tests showed that compounds 7b and 7i possessed certain anti-tobacco mosaic virus activity. 相似文献
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2‐Alkyl and 2‐arylhydrazine derivatives of 5H‐2‐R‐6‐fluoro‐7‐methyl‐1,3,4‐thiadiazolo[3,2‐a]pyrimidin‐5‐one were prepared by reaction of 5H‐2‐bromo‐6‐fluoro‐7‐methyl‐1,3,4‐thiadiazolo[3,2‐a]pyrimidin‐5‐one with hydrazine derivatives. A convenient procedure was developed for the preparation of new hydrazine derivatives of 5H‐2‐R‐6‐fluoro‐7‐methyl‐1,3,4‐thiadiazolo[3,2‐a]pyrimidin‐5‐one. J. Heterocyclic Chem., (2011). 相似文献
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Electrochromism has been demonstrated by three novel electrochemically-reversible compounds and, which were synthesised by Pd catalysed cross-coupling of iodotrimethylTTF (6) and 2,6(7)-diiodoTTF (7) with the 2,5-diaryl-1,3,4-oxadiazole derivatives 1 and 2 containing terminal ethyne and butadiyne groups. 相似文献
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Andrea Santagati Maria Santagati Filippo Russo Giuseppe Ronsisvalle 《Journal of heterocyclic chemistry》1988,25(3):949-953
Continuing earlier studies designed to obtain derivatives of 1,3,4-thiadiazolo[3,2-a]pyrimidin-5-one and of the isomeric 7-one of pharmacological interest, some novel compounds 2 and derivatives of 6,7,8,9-tetrahydro-5H-1,3,4-thiadiazolo[2,3-b]quinazolin-5-one ( 3 ) were prepared. Derivatives of pyrimido[2,1-b]benzothiazol-2-one ( 6 ) and of the isomeric 4-one derivatives 8 were also synthesized. Structural identification was obtained by 1H-nmr, ir and mass spectra. 相似文献
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5-Aryl(or benzyl)-3-(2-bromoethyl)-1,3,4-oxadiazol-2(3H)-ones 3 have been prepared. They were reacted with secondary alkylamines without any change of the heterocycle to give amino derivatives 6 , but with primary alkylamines, cyclic transformation occurred to give 1-acylamino-3-alkylimidazolidin-2-ones 7 . In the presence of sodium alcoholate, bromo compounds 3 were transformed into 2-aryl(or benzyl)-4-alkoxycarbonyl-5,6-dihydro-4H-1,3,4-oxadiazines 9 . 相似文献
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The 1 : 1 imine intermediate 7 generated by the addition of a primary amine 2 to chloroacetone ( 1 ) is trapped by (isocyanoimino)triphenylphosphorane ( 4 ) in the presence of an aromatic carboxylic acid 3 and leads to the formation of the corresponding iminophosphorane intermediate 9 (Scheme 2). The 1,3,4‐oxadiazole derivatives 5 are then formed via an intramolecular aza‐Wittig reaction of the iminophosphorane intermediate 9 . The reactions were completed under neutral conditions at room temperature. The fully substituted 1,3,4‐oxadiazole derivatives 5 were produced in high yields (Table). 相似文献
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In this study, certain 3‐substituted styrylquinoxalin‐2(1H)‐ones ( 2a‐d ) and their 2‐chloro ( 3a‐d ) and 2‐piperazinyl derivatives ( 4a‐g ) were synthesized from 3‐methylquinoxalin‐2(1H)‐one ( 1 ). In addition, a series of 1‐alkyl‐3‐substituted styrylquinoxalin‐2(1H)‐ones ( 5a‐d ) was also prepared. Moreover, 3‐(N2‐arylidenehydrazinocarbonyl)quinoxalin‐2(1H)‐ones ( 8a‐c ) as well as their cyclized oxadiazolinyl derivatives ( 9a‐c ) were prepared from 3‐hydrazinocarbonylquinoxalin‐2(1H)‐one ( 7 ). Furthermore, 3‐(5‐substituted thio‐1,3,4‐oxadiazol‐2‐yl)quinoxalin‐2(1H)‐ones ( 11a‐c ) and ( 12a‐c ) were obtained from the intermediate compound ( 10 ) ‐ previously obtained via cyclization of ( 7 ) with CS2. Likewise, 3‐(5‐oxo‐4,5‐dihydro‐(1,3,4‐oxadiazol‐2‐yl)quinoxalin‐2(1H)‐one ( 13 ), 3‐[5‐(4‐nitrophenyl)‐1,3,4‐oxadiazol‐2‐yl]‐quinoxalin‐2(1H)‐one ( 14 ) and its 2‐chloro derivative ( 15 ) were prepared from 3‐hydrazinocarbonylquinoxalin‐2(1H)‐one ( 7 ). Some of these derivatives were evaluated for antimicrobial activity in vitro and some of the tested compounds showed antibacterial or antifungal activity. 相似文献