共查询到18条相似文献,搜索用时 125 毫秒
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5,7-二甲基-1,2,4-三唑并[1,5-a]嘧啶-2-甲酰腙类化合物的合成与生物活性 总被引:6,自引:0,他引:6
以5-氨基-1H-1,2,4-三唑-3-羧酸为起始原料, 设计合成了13个新型的5,7-二甲基-1,2,4-三唑并[1,5-a]嘧啶-2-甲酰腙类化合物, 通过1H NMR, MS和元素分析对所合成的化合物进行了结构表征. 初步的生物活性测试结果表明, 所合成的化合物均表现出不同程度的除草及杀菌活性, 其中化合物4b, 4h和5m的活性较好, 在50 mg/L浓度下对水稻纹枯病菌的抑制率达90 %以上. 相似文献
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以5-氨基-1H-1,2,4-三唑-3-羧酸乙酯为起始原料, 设计合成了11个新型的2-取代硫醚-5-(5,7-二甲基-1,2,4-三唑并[1,5-a]嘧啶基)-1,3,4-噁二唑类化合物(5)和6个新型的2-取代硫醚-5-(5,7-二甲基-1,2,4-三唑并[1,5-a]嘧啶基)-1,3,4-噻二唑类化合物(8). 通过1H NMR, MS和元素分析对所合成的化合物进行了结构表征. 初步的生物活性测试结果表明, 所合成的化合物均表现出不同程度的除草及杀菌活性, 其中化合物5k和8f的活性最好, 在50 mg/L浓度下对水稻纹枯病菌的抑制率达90%以上. 相似文献
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以2-溴丙酸甲酯、α,α-二氯甲基甲醚和胍唑为原料, 经缩合以及环化反应制得2-氨基-6-甲基-5-氧代-4,5-二氢-1,2,4-三氮唑并[1,5-a]嘧啶. 为了提高其在有机溶剂中的溶解性, 该化合物再同1-溴丁烷发生亲核取代反应得到了2-氨基-6-甲基-5-氧代-4-正丁基-4,5-二氢-1,2,4-三氮唑并[1,5-a]嘧啶, 然后与芳基醛和叔丁基异氰发生Ugi多组分反应, 合成了一系列具有潜在催吐活性的2-取代氨基-6-甲基-5-氧代-4-正丁基-4,5-二氢-1,2,4-三氮唑并[1,5-a]嘧啶类衍生物, 产品结构经质谱、核磁共振谱及元素分析确认. 相似文献
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1,3-双[3-芳基-1,2,4-三唑并[3,4-b]-1,3,4-噻二唑-6-基]丙烷类化合物的合成 总被引:1,自引:0,他引:1
戊二酸(1)与3-芳基-4-氨基-5-巯基-1,2,4-三唑(2a~2o)在相转移催化剂四丁基碘化铵和POCl3作用下, 高收率合成了一系列新的1,2-双[3-芳基-1,2,4-三唑并[3,4-b]-1,3,4-噻二唑-6-基]丙烷(3a~3o). 其结构经IR, 1H NMR, MS和元素分析确证. 相似文献
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通过氮杂Wittig反应合成了一系列结构新颖的未见文献报道的取代四氢苯并[4',5']噻吩并[3',2':5,6]吡啶并[4,3-d]嘧啶-4(3H)-酮化合物6, 产物的结构通过核磁共振氢谱、质谱、红外光谱、元素分析的确证. 为进一步了解此类化合物的结构, 对化合物6c进行了X射线单晶衍射. 初步杀菌活性测定结果表明, 该类化合物具有较好的杀菌活性和选择性. 如6f在50 mg/L浓度时, 对黄瓜灰霉菌的抑制率为98%. 相似文献
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合成了5-取代-1,2,4-三唑并[4,3-a]喹唑啉衍生物2a~2q.利用最大电惊厥法(MES)和旋转棒法(Rotarod Test),以小鼠腹腔给药,分别测定了其抗惊厥活性和神经毒性.药理实验结果表明,化合物5-正庚氧基-1,2,4-三唑并[4,3 -a]喹唑啉(2d)的抗惊厥活性最强,其半数有效量EDso为19.7 mg/kg,保护指数PI为6.2.由化学物质诱发的抗惊厥实验结果表明,化合物2d能对抗由戊四唑、异烟肼、硫代氨基脲和3-巯基丙酸诱发的惊厥作用,推测其抗惊厥作用是通过增强γ-aminobutyric acid (GABA)神经能系统和活化谷氨酸脱羧酶或抑制GABA转氨酶而起抗惊厥作用. 相似文献
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Feng-Yu Piao Cheng-Xi Wei Rong-Bi Han Wen-Bin Zhang Wei Zhang Ri-Shan Jiang 《合成通讯》2013,43(16):2337-2345
A series of novel 9-alkoxy-6,7-dihydro-2H-benzo[c][1,2,4]triazolo[4,3-a]azepin-3(5H)-one derivatives was designed and synthesized starting from 2,3,4,5-tetrahydro-7-hydroxy-1H-2-benzazepin-1-one. The structures of these compounds were confirmed by mass, 1H NMR infrared spectra, and elemental analysis. Their anticonvulsant activity was evaluated by maximal electroshock (MES) test, and their neurotoxic effects were determined by the rotarod neurotoxicity test. The results shown that 3k was the most active compound with median effective dose (ED50) of 27.3 mg/kg, median toxicity dose (TD50) of 118.3 mg/kg, and protective index (PI) of 4.3. Possible structure–activity relationship is discussed. 相似文献
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The regioselective synthesis of cis and trans stereoisomers of variously functionalized octahydro[1,2,4]triazolo[4,3-a]quinazolin-5-ones was performed. The 2-thioxopyrimidin-4-ones used in the synthesis reacted with hydrazonoyl chlorides in a regioselective manner to produce the angular regioisomers [1,2,4]triazolo[4,3-a]quinazolin-5-ones rather than the linear isomers [1,2,4]triazolo[4,3-a]quinazolin-5-ones. The synthesis process took place with electronic control. The angular regiochemistry of the products was confirmed by X-ray experiments and two-dimensional NMR studies. 相似文献
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Andrey V. Khramchikhin Mariya A. Skrylnikova Iana L. Esaulkova Ekaterina O. Sinegubova Vladimir V. Zarubaev Maxim A. Gureev Aleksandra M. Puzyk Vladimir A. Ostrovskii 《Molecules (Basel, Switzerland)》2022,27(22)
This study of the interaction system of binucleophilic 3-substituted 4-amino-4H-1,2,4-triazole-5-thiols and 3-phenyl-2-propynal made it possible to develop a new approach to synthesis of such isomeric classes as 7-benzylidene-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine and 8-phenyl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazepine. Among the 20 compounds studied in vitro against influenza A/Puerto Rico/8/34 (H1N1) virus, half of them demonstrated selectivity index (SI) of 10 or higher and one of them (4-((3-phenylprop-2-yn-1-yl)amino)-4H-1,2,4-triazole-3-thiol) possessed the highest (SI > 300). Docking results and values showed that the preferred interactant for our ligands was M2 proton channel of the influenza A virus. Protein-ligand interactions modeling showed that the aliphatic moiety of ligands could negatively regulate target activity level. 相似文献
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α-四氢萘酮的乙氧羰基腙(1)经LTA氧化,得到α-偶氮-α-乙酰氧基化合物2.在A lC l3作用下,化合物2脱去乙酰氧基产生重氮正离子中间体3,再经与腈的1,3-偶极环加成、[1,2]-迁移扩环、碱性水解和与苦味酸作用,得到新型[1,2,4]-三唑并[1,5-a][1]苯并氮杂苦味酸盐6a~6c.以2,3-二氢-1-茚酮为底物,采用相同的合成路线,合成了1,2,4-三唑并[1,5-a]-二氢喹啉苦味酸盐12a~12c. 相似文献
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新型环烷烯并嘧啶并噻唑-3-酮类化合物的合成 总被引:1,自引:0,他引:1
以环戊酮、环庚酮为起始原料合成的环烷烯并[1,2-d]嘧啶-2-硫酮(2)与氯乙酸、芳香醛反应, 合成具有潜在抗癌活性的稠合杂环化合物5-芳基-2,8-二芳亚甲基-2,3,6,7-四氢-5H,8H-环戊烯并[1,2-d]噻唑并[3,2-a]嘧啶-3-酮(3)以及5-芳基-2,10-二芳亚甲基-2,3,6,7,8,9-六氢-5H,10H-环庚烯并[1,2-d]噻唑并[3,2-a]嘧啶-3-酮(4). 3和4的结构经1H NMR, IR, MS分析确认. 相似文献
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A straightforward method has been developed for the synthesis of 1-phenyl-imidazo [2,1-c][1,2,4]triazole derivatives 5a–j and 1-phenyl-[1,2,4]triazolo[4,3-a]pyrimidinones derivatives 6a–g starting from 5-amino-1-phenyl[1,2,4]triazole and p-toluenesulfonic acid (PTSA). This methodology affords a number of 1-phenyl-imidazo [2,1-c][1,2,4]triazoles 5a–j and 1-phenyl-[1,2,4]triazolo[4,3-a]pyrimidinones 6a–g in reasonable yields and short reaction times. The structures of all new compounds were elucidated using infrared, 1H and 13C NMR, and high-resolution mass spectrometry. Some of the newly synthesized compounds were screened for their antimicrobial activity.
[Supplementary materials are available for this article. Go to the publisher's online edition of Synthetic Communications ® for the following free supplemental resource(s): Full experimental and spectral details.] 相似文献