共查询到19条相似文献,搜索用时 78 毫秒
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含1,3,4-噻二唑环吡唑并[3,4-d]嘧啶类化合物的合成及生物活性 总被引:1,自引:0,他引:1
通过5-氨基-4-氰基-1-苯基吡唑与甲酸发生环合、再经氯化和芳香族亲核取代反应,合成了12种新的含1,3,4-噻二唑环吡唑并[3,4-d]嘧啶类化合物.目标化合物的结构经红外光谱、核磁共振氢谱、质谱和元素分析方法予以确认.初步的生物活性测定试验表明,在50 mg/L浓度下,大部分目标化合物对小麦纹枯病菌(Rhizoctonia cerealis)表现出较好的杀菌活性,其中化合物5b,5d和5j的抑菌率超过90%. 相似文献
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通过6-氨基嘧啶、取代苯甲醛与丙二腈的三组分反应合成了4种吡啶并[2,3-d]嘧啶受体分子,利用紫外-可见吸收光谱考察了其与F-,Cl-,Br-,AcO-,4HSO-,2 4H PO-等阴离子的作用.结果表明该类受体分子与阴离子形成氢键配合物,导致吡啶并[2,3-d]嘧啶受体的光谱发生变化.测定了配合物的结合比和稳定常数,发现受体化合物对AcO-离子具有良好的选择性,对其它多种阴离子无影响.Job曲线表明受体分子与阴离子间形成1∶1型的配合物.1H NMR滴定进一步证实了氢键作用的存在及参与类型. 相似文献
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以环己酮为原料,利用Gewald反应合成了6个3-烷基-5,6,7,8-四氢苯并[4,5]噻吩并[2,3-d]嘧啶-4-酮衍生物和17个3-亚苄基胺基四氢苯并[4,5]噻吩并[2,3-d]嘧啶-4-酮衍生物,通过1H NMR、13C NMR、IR和MS对所合成的化合物进行了结构表征,并对所合成化合物进行了抗肿瘤活性的筛选.结果表明4个化合物对人鼻咽癌细胞株(KB)和鼻咽鳞癌细胞株(CNE2)两种肿瘤细胞株表现出一定程度的抑制活性. 相似文献
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利用L-脯氨酸催化的5-氯水杨醛(1)与6-甲基-4-羟基吡喃酮(2)的缩合反应及硫酸铜催化下与1,3-二甲基-5-氨基吡唑(3)的串联反应,合成得到了10-氯-1,3-二甲基-5-(2-氧代丙基)色烯并[4,3-d]吡唑并[3,4-b]吡啶-6(3H)-酮(4)和10-氯-5-二乙氧基甲基-1,3-二甲基色烯并[4,3-d]吡唑并[3,4-b]吡啶-6(3H)-酮(5).化合物5的结构通过单晶X射线衍射法确定:晶体属于三斜晶系,空间群P-1;相对分子质量Mr=803.68;晶胞参数a=1.03160(10)nm,b=1.42900(13)nm,c=1.44268(15)nm;V=1.9448(3)nm~3;Z=2;晶胞密度Dc=1.372g/cm~3;吸收系数μ=0.228mm-1;单胞中电子的数目F(000)=840.晶体结构用直接法解出,经全矩阵最小二乘法对原子参数进行修正,最终的偏离因子为R=0.0681,w R=0.2051.在晶体结构中色烯环与吡啶环及吡唑环近似于共平面. 相似文献
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Eman M. Othman Amany A. Bekhit Mohamed A. Anany Thomas Dandekar Hanan M. Ragab Ahmed Wahid 《Molecules (Basel, Switzerland)》2021,26(10)
The present study reports the synthesis of new purine bioisosteres comprising a pyrazolo[3,4-d]pyrimidine scaffold linked to mono-, di-, and trimethoxy benzylidene moieties through hydrazine linkages. First, in silico docking experiments of the synthesized compounds against Bax, Bcl-2, Caspase-3, Ki67, p21, and p53 were performed in a trial to rationalize the observed cytotoxic activity for the tested compounds. The anticancer activity of these compounds was evaluated in vitro against Caco-2, A549, HT1080, and Hela cell lines. Results revealed that two (5 and 7) of the three synthesized compounds (5, 6, and 7) showed high cytotoxic activity against all tested cell lines with IC50 values in the micro molar concentration. Our in vitro results show that there is no significant apoptotic effect for the treatment with the experimental compounds on the viability of cells against A549 cells. Ki67 expression was found to decrease significantly following the treatment of cells with the most promising candidate: drug 7. The overall results indicate that these pyrazolopyrimidine derivatives possess anticancer activity at varying doses. The suggested mechanism of action involves the inhibition of the proliferation of cancer cells. 相似文献
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Zeinab H. Ismail Soad M. Abdel-Gawad Anhar Abdel-Aziem M. M. Ghorab 《Phosphorus, sulfur, and silicon and the related elements》2013,188(8):1795-1805
A novel series of the pyrazolo[3,4-d]pyrimidines having biologically active sulfur moieties 3-20 were prepared via reaction of 4-mercapto-1-phenyl-1 H -pyrazolo[3,4-d]pyrimidine 3 with different reagents. Identification of the new compounds was established by elemental analyses, IR, 1 H-NMR, and mass spectral data. Some of the obtained compounds showed the interesting antimicrobial activity comparable to antibiotic chloramphenicol as standard antibacterial agent and Terbinafin as a standard antifungal agent. 相似文献
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A. H. Shamroukh A. E. Rashad H. H. Sayed 《Phosphorus, sulfur, and silicon and the related elements》2013,188(10):2347-2360
Abstract A novel β -enaminonitrile of 1-(6-p-tolyl-pyridazin-3-yl)-pyrazole derivative 2 was formed using (6-p-tolyl-pyridazin-3-yl)-hydrazine ( 1 ) and 2-ethoxymethylenemalononitrile. The β-enaminonitrile derivative 2 was in turn used as a precursor for the preparation of pyrazoles ( 4 , 6 ), pyrazolo[3, 4-d]-pyrimidines ( 3 , 7–12 ) and pyrazolo[4, 3-e][1,2,4]triazolo[4,3-c]pyrimidine ( 13 ). Also, N- and S-acyclic nucleosides 14 and 15 were prepared. Some of the prepared products showed potent antimicrobial activity. 相似文献
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A new synthesis of 4-methoxy (or ethoxy)-1,6-diaryl-1H-pyrazolo[3,4-d]pyrimidine derivatives is described. An efficient one-step methodology for the title compounds was achieved by using 5-amino-1-aryl-1H-pyrazole-4-carbonitriles with arylaldehydes in CH3OH or C2H5OH and NaOH at 60 °C. The new compounds were obtained in moderate to good yields as stable solids and easily purified by filtration. 相似文献
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Several pyrazolo[3,4-b]pyridine (3,4) and pyrazolo-[3,4-d]pyrimidine (5-13) derivatives were prepared using 5-amino-l-(5-ethyl-5H-1,2,4-triazino[5,6-b]-indol-3-yl)-lH-pyrazole-4-carbonitrile (2) . The pyridine derivatives 3 and 4 were obtained by reaction of 2 with malononitrile and ethyl cyanoacetate, respectively, while pyrimidine analogs 5-13 were synthesized cither by a one-step or multi-step sequence. 相似文献
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M. Yu. Onysko O. V. Svalyavin A. V. Turov V. G. Lendel 《Chemistry of Heterocyclic Compounds》2008,44(7):872-875
The reaction of 4-imino-1-methyl-5-phenyl-6-propargylthio-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidine with halogens leads to
the formation of (Z)-8-halomethylene-4-imino-1-methyl-5-phenyl-4,5,7,8-tetrahydro-1H-pyrazolo[4,3-e][1,3]thiazolo[3,2-a]pyrimidinium
trihalide.
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Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 7, pp. 1085–1088, July, 2008. 相似文献
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3-Ethoxycarbonyl-5-methyl-1-(4-methylphenyl)-4-pyrazoloylhydroximoyl chloride (1) reacted with o-phenylenediamine, o-aminothiophenol, o-aminophenol and methyl anthranilate to afford 3-nitrosoquinoxaline, benzothiadiazine, benzoxadiazine, and 3-hydroxyquinazoline, respectively. Imidazo[1,2-a]pyridine, imidazo[1,2-a]pyrimidine and isoxazole derivatives were obtained via the reaction of 1 with 2-aminopyridine, 2-aminopyrimidine and the appropriate active methylene compounds, respectively. Pyrazolo[3,4-d]pyridazines, and pyrrolidino[3,4-d]isoxazolines derivatives were also synthesized. The structures of the newly synthesized compounds were established on the basis of spectral data and alternate synthesis whenever possible. 相似文献
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A novel series of pyrazolo[1,5-a]pyrimidines 14a–j and pyrazolo[1,5-a]quinazolines 18a, b were synthesized via condensation of 5-amino-1H-pyrazoles 10a, b with 3-(dimethylamino)-1-aryl-prop-2-en-1-ones 11a–e and 2-((dimethylamino)methylene)-5,5-dimethylcyclohexane-1,3-dione (15), respectively, in glacial acetic acid. Finally, treatment of 10a, b with sodium nitrite (NaNO2) afforded pyrazolo[3,4-d]triazines 20a, b. Structures of compounds were confirmed by their spectral data. These compounds were screened for their in vitro cytotoxic activities against human cancer cell lines (HepG-2 and MCF-7) using 3-[4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay. The results reveal that, the compounds 14b and 14h were the most potent in comparison with doxorubicin. The structure–activity relationship was discussed. 相似文献