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1.
《Journal of heterocyclic chemistry》2017,54(2):850-858
7‐Amino‐3‐phenyl‐[1,2,4]triazolo [4,3‐a] pyrimidin‐5(1H )‐one ( 5 ) was utilized as key intermediate for the synthesis of some new, quinolines 9 , 10 , 11 , 12 , 13 , 14 and 18 , 19 , 20 , acrylonitrile 25 and 28 , coumarin 26 , and pyrazoles 31 , 32 , 33 , 34 incorporating triazolopyrimidines. The structures of the newly synthesized compounds were confirmed by elemental analysis, IR, 1H NMR, and mass spectral data. Representative compounds of the synthesized products were tested and evaluated as antimicrobial. Compounds 25 , 28 , 31 , 32 , 33 , and 34 are the most promising. 相似文献
2.
The novel 2-(1H)-pyridone, the lead compound of the pyridone derivative 1, reacted with an electrophilic reagent (ethyl chloroacetate) to give the corresponding ester 2. Condensation of compound 2 with thiosemicarbazide and/or hydrazine hydrate afforded the mercaptotriazole and the corresponding acetic acid hydrazide derivatives 3 and 4, respectively. The latter compound reacted with ethyl acetoacetate, ethyl cyanoacetate, and maleic anhydride to give compounds 5, 6, and 7, respectively. Alkylation of compound 3 with methyl iodide or chloroacetic acid afforded methylsulfanyltriazole and thiazolotriazole derivatives 8 and 9, respectively. Compound 8 reacted with glycine to afford the imidazotriazole derivative 10. Both compounds 9 and 10 reacted with glucose and benzaldehyde to give compounds 11, 12, 13, and 14, respectively. Some of the prepared products were selected and subjected to screening for their antioxidant activity. 相似文献
3.
Synthesis of Some New Fused Pyrazole Derivatives Bearing Indole Moiety as Antioxidant Agents 下载免费PDF全文
Ahmed El‐Mekabaty Hassan A. Etman Ahmed Mosbah 《Journal of heterocyclic chemistry》2016,53(3):894-900
3‐(1H‐Indol‐3‐yl)‐1H‐pyrazol‐5‐amine 3 was prepared in a quantitative yield by heating 3‐(1H‐indol‐3‐yl)‐3‐oxopropanenitrile 2 in dry ethanol with hydrazine hydrate, and utilized as key intermediate for the synthesis of some new pyrazolo[1,5‐a]pyrimidines and pyrazolo[5,1‐c]triazines. Structures of the newly synthesized compounds were established by elemental analysis and spectral data and evaluated as antioxidant agents. Most of the tested compounds belonging to the pyrazolo[1,5‐a]pyrimidine series exhibited better activities than members of the pyrazolotriazine one. 相似文献
4.
《Journal of heterocyclic chemistry》2017,54(1):268-277
As a part of ongoing studies in developing new potent antioxidant agents, N‐[4‐(aminosulfonyl)phenyl]‐2‐cyanoacetamide ( 3 ) was utilized as key intermediate for the synthesis of some new thiophene, chromene, and pyrazolotriazine pyridine derivatives. The structures of the newly synthesized compounds were confirmed by elemental analysis, IR, 1H‐NMR, and mass spectral data. Representative compounds of the synthesized products were tested and evaluated as antioxidant. Compounds 7 and 30 are promising compounds. 相似文献
5.
Elasasy M. E. A. Elnaggar D. H. Hafez N. A. Abdel Azab M. E. Amr A. E. Omran M. M. Mohamed A. M. 《Russian Journal of General Chemistry》2021,91(5):915-925
Russian Journal of General Chemistry - Some new fluoro-heterocyclic compounds containing thiazole and pyridine moities have been synthesized and studied for their antiproliferative activity.... 相似文献
6.
查尔酮是一类具有多种生物活性的1,3-二苯基丙烯酮化合物.以4-氟苯乙酮和2-噻吩甲醛为原料出发,经取代、Aldol反应和衍生化,合成得到16个未见文献报道的含哌嗪片段的噻吩查尔酮衍生物.以氧氟沙星、左氧氟沙星、莫西沙星作阳性对照,采用K-B纸片扩散法测试了目标化合物对金黄色葡萄球菌(Staphylococcus aureus Rosenbach)、大肠埃希菌(Escherichia coli)和枯草芽孢杆菌(Bacillus subtilis)的抑菌活性.结果表明,(E)-1-[4-(4-肉桂酸甲酯甲基哌嗪基)苯基]-3-(噻吩-2-基)丙-2-烯酮(4b)和(E)-1-{4-[4-(2-氧亚基苯乙基)哌嗪基]苯基}-3-(噻吩-2-基)丙-2-烯酮(4e)对枯草芽孢杆菌高度敏感,且最低抑菌浓度为4.0μg/m L. 相似文献
7.
Romuald Skowroński Grzegorz Grabowski Jarosław Lewkowski 《Phosphorus, sulfur, and silicon and the related elements》2013,188(1)
Abstract Synthesis of a series of 1 -aminoalkanephosphonic acids bearing hran moiety was performed, starting from the preparation[I] of various N-substituted aminophosphonic esters. We were encouraged by previous Boduszek's study [2]. 相似文献
8.
Prasad Mutyala Veera Venkata Vara Rao Radha Hunasenahalli Raghavendra Veeranna Vadde Chennupalli Venkata Suryanarayana Sathish Byrappa 《Russian Journal of General Chemistry》2021,91(12):2522-2526
Russian Journal of General Chemistry - Novel quinolone derivatives have been designed and readily synthesized according to a simple protocol including O-alkylation and Claisen rearrangement... 相似文献
9.
为了发现具有良好生物活性的吡唑肟化合物,以唑螨酯为先导化合物,在吡唑肟中引入取代噁唑结构,设计并制备了20个未见文献报道的新型吡唑肟衍生物,利用1H NMR,13C NMR和元素分析确证了目标产物的结构.生物活性测试结果显示,部分目标化合物在500和100μg/mL浓度下对粘虫或蚜虫表现出优良的杀虫活性,其中5-(3-氟苯氧基)-1,3-二甲基-1H-吡唑-4-甲酰基-O-{[5-(4-氯苯基)噁唑-2-基]甲基}肟(9j)、5-(4-氟苯氧基)-1,3-二甲基-1H-吡唑-4-甲酰基-O-{[5-(4-氯苯基)噁唑-2-基]甲基}肟(9k)、5-(4-叔丁基苯氧基)-1,3-二甲基-1H-吡唑-4-甲酰基-O-{[5-(4-氯苯基)噁唑-2-基]甲基}肟(9r)和5-(4-甲氧基苯氧基)-1,3-二甲基-1H-吡唑-4-甲酰基-O-{[5-(4-氯苯基)噁唑-2-基]甲基}肟(9s)在浓度为100μg/mL时对粘虫的防治效果均达100%,5-(4-溴苯氧基)-1,3-二甲基-1H-吡唑-4-甲酰基-O-{[5-(4-氟苯基)噁唑-2-基]甲基}肟(9g)和9s在浓度为100μg/mL时对蚜虫的杀灭活性均为100%.此外,化合物9s在500μg/mL时对朱砂叶螨的防治效果为70%. 相似文献
10.
Nuray Ulusoy Öznur Ateş Ömer Küçükbasmacı Muammer Kiraz Yıldız Yeğenoğlu 《Monatshefte für Chemie / Chemical Monthly》2003,134(3):465-474
Summary. Some novel 4-[[2-[[5-(2-furanyl)-4-alkyl/aryl-4H-1,2,4-triazol-3-yl]thio]-acetyl/propionyl]-amino]-1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazoles were synthesized and evaluated for in vitro antibacterial activity against Staphylococcus aureus ATCC 29213, Pseudomonas aeruginosa ATCC 27853, Escherichia coli ATCC 25922, and Enterococcus faecalis ATCC 29212 and antifungal activity against Candida albicans ATCC 10231, Candida parapsilosis ATCC 22019, Candida krusei ATCC 6258, Candida parapsilosis, Trichophyton mentagrophytes var. erinacei NCPF 375, Microsporum gypseum NCPF 580, and Trichophyton rubrum using the microbroth dilution method. All of the compounds were found to be ineffective against the above bacteria within
the applied MIC ranges. On the other hand, they were effective against fungi to different degrees. Three compounds showed
high activity against C. parapsilosis and T. mentagrophytes var. erinacei NCPF 375 (MIC = 8 μg cm−3). The in vitro antimycobacterial activity of the new compounds was also investigated against Mycobacterium tuberculosis H37RV (ATCC 27294) in BACTEC 12B medium using a broth microdilution assay, the Microplate Alamar Blue Assay (MABA). Compounds
exhibiting fluorescence were tested in the BACTEC 460 radiometric system. The most active compound was found with 66% inhibition
at >6.25 μg cm−3.
Corresponding author. E-mail: nurayulusoy@yahoo.com
Received July 24, 2002; accepted August 26, 2002 相似文献
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Some compounds containing oxime type such as fenpyroximate have good activity used as pesticide. In order to discover new lead, the novel compound (Ⅰ-Ⅴ) were designed and synthesized. Their structures were confirmed by IR, 1HNMR and MS. 相似文献
13.
Hai Shi Fang-Ming Liu Song-Wei Shen 《Phosphorus, sulfur, and silicon and the related elements》2013,188(2):263-270
Abstract A series of novel 3-aryl-5-(2-aryl-1,2,3-triazol-4-yl)-1-(4-aryl-2-thiazoyl)-pyrazolines 6a–6r were synthesized using 2-aryl-4-formyl-1,2,3-triazoles 1a,b as the starting materials. Thus, reacting 1a,b with 1-arylethanones 2a–2c gave 1-aryl-3-(2-aryl-1,2,3-triazol-4-yl)-2-propen-1-ones 3a–3f. The reaction of the latter with thiosemicarbazide afforded 3-aryl-5-(2-aryl-1,2,3-triazol-4-yl)-1-thiocarbamoyl-pyrazolines 4a–4f, which condensed with 2-bromo-1-arylethanones 5a–5c to afford the target compounds 6a–6r. The chemical structures of the compounds were verified by means of their IR, 1H NMR, ESI-MS spectroscopic data, and elemental analysis. Supplemental materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements to view the free supplemental file. GRAPHICAL ABSTRACT 相似文献
14.
Novel Quinazoline Derivatives Bearing a Sulfapyridine Moiety as Anticancer and Radiosensitizing Agents 下载免费PDF全文
Mostafa M. Ghorab Fatma A. Ragab Helmi I. Heiba Ahmad A. Bayomi 《Journal of heterocyclic chemistry》2014,51(Z1):E255-E262
Quinazoline derivatives posses many types of biological activities and have recently been reported to show substantial antitumor activity in vitro and/or in vivo. There is a variety of mechanisms for their anticancer activity. The present work reports the possible utility of methyl anthranilate in the synthesis of some new quinazoline derivatives, bearing a substituted sulfonamide moiety. All the newly synthesized compounds were evaluated for their in vitro anticancer activity against human liver cancer cell line, using doxorubicin as a reference drug. In addition, the most active compounds 14 and 15 were selected and evaluated for their ability to enhance the cell killing effect of γ‐radiation. 相似文献
15.
Synthesis and Antioxidant Activity of Some New Binary Pyrazoles Containing Core Phenothiazine Moiety
《Journal of heterocyclic chemistry》2017,54(2):1369-1377
α,β‐Unsaturated ketones containing phenothiazine moiety 4 , 5 , and 7 were synthesized by condensation of 2‐acetylphenothiazine ( 1 ) with different aryl aldehydes 2 , 3 and dimethylformamide dimethylaceal. Pyrazoles 11 , 18 , 20 , 22 , 23 , 24 , 25 , 26 , 28 , 29 , 31 , 32 and oxazole 34 skeletons were also synthesized by 1,3‐dipolar cycloaddition reactions of α,β‐unsaturated ketones with different nucleophilic reagents. Formylpyrazole derivative 36 was synthesized through Vilsmeier–Haack reaction of phenylhydrazone 35b . Newly synthesized compounds were screened for antioxidant activity. The data showed clearly that most of the compounds anchored to phenothiazine moiety displayed good antioxidant activity using ABTS method. Furthermore, compounds 11 , 14 , and 28 exhibited high protection against DNA damage induced by the bleomycin iron complex. 相似文献
16.
Yitao Li Wenqiang Yao Jian Lin Falin Li Yang Wu Junxing Xu 《Journal of heterocyclic chemistry》2019,56(8):2170-2178
The triazole sulfonamide played a very important role in the field of research of new agrochemical compounds as a novel heterocyclic compound with lack of reported resistance. For the research on the innovative triazole sulfonamide fungicide effective against cucumber downy mildew (CDM), the present article designed an array of 1,2,4‐triazole‐1,3‐disulfonamide derivatives. The derivatives were synthesized via coupling multiple benzylamine with triazole sulfonamide groups. 1H‐NMR, 13C‐NMR, and LC–MS spectrometry were used to characterize these synthesized compounds. Most of these derivatives exhibited better fungicidal activities than that of the commercial cyanosole using bioassays. In particular, compounds 6g and 6h showed the best fungicidal activity against CDM (EC50 = 6.91 and 10.62 mg/L). Comparative experiments demonstrated that the fungicidal activity of 6g and 6h was better than the commercial pesticides amisulbrom and cyanosole. According to the study, the compound 6g had a giant application potential on fungicide against CDM. 相似文献
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18.
M. K. Samota A. Kumar J. Kaur S. Mittal Gita Seth 《Phosphorus, sulfur, and silicon and the related elements》2013,188(8):1919-1924
The phosphorylation of 2-(2′-hydroxyphenyl) benzoxazole has been accomplished with phosphorus oxychloride in a 1:1, 2:1, and 3:1 molar ratio in the presence of a base to yield O-phosphorylated benzoxazole derivatives. Their structures were confirmed by elemental analyses and IR, 1H NMR, and 31P NMR spectral studies. These compounds have been screened for their insecticidal activity against Periplenata americana and were found to be quite active in this respect. 相似文献
19.
Kiran K. Sarasija M. Ananda Rao Boddu Namratha V. Ashok D. Srinivasa Rao A. 《Russian Journal of General Chemistry》2019,89(9):1859-1866
Russian Journal of General Chemistry - A series of novel 1,4-substituted bis-aralkyl and aryl 1,2,3-triazoles bearing thiophene chalcones are synthesized via the Claisen condensation of bis... 相似文献
20.
A series of novel benzothiazole derivatives bearing semicarbazone as a linker was designed and synthesized, and their in vitro antitumor activities were evaluated against four cancer cell lines(HT29, H460, A549 and MDA-MB-231). Most of them showed moderate to excellent activity against all the tested cell lines. Among them, compounds 12a―12i with fluoro-substituted benzyl-1H-indole moiety displayed more potent activity than those with phenyl moiety. The most promising compound 12d exhibited excellent antitumor activity with IC50 values of 0.015, 0.28, 1.53 and 0.68 μmol/L against the four tested cell lines respectively. 相似文献