共查询到19条相似文献,搜索用时 218 毫秒
1.
为了寻找毒性低、增敏作用强的乏氧细胞放射增敏剂,设计并合成了一系列5-溴-,5-甲基-,和5-未取代的3-硝基-1,2,4-三唑-1-乙酰胺类化合物,用HeLaS3细胞进行了体外试验。结果表明5-溴取代衍生物的增敏作用强于相应的5-甲基-或5-未取代的硝基三唑衍生物,但是它们的毒性亦增大。修饰1位乙酰胺侧链也可以改变化合物的增敏作用和亲脂性。在所测定的化合物中TA-101[2-(3-硝基-1-三唑基)乙酰胺]由于有高的增敏作用和低亲脂性,可能是一个有希望的放射增敏剂。 相似文献
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卟啉硝基咪唑类衍生物的合成及放射增敏作用 总被引:2,自引:0,他引:2
目的设计合成卟啉硝基咪唑类化合物,评价其体外肿瘤放射增敏活性,寻找新的肿瘤放射增敏剂。方法以吡咯、苯甲醛、硝基咪唑为原料,经环合、溴代、取代、络合等反应合成卟啉硝基咪唑类化合物及其金属配合物。采用MTT法考查该系列衍生物对人宫颈癌Helo细胞株的放射增敏活性。结果合成了12个未见文献报道的新化合物,其结构经紫外光谱、ESI质谱、红外光谱和核磁共振氢谱确证。在4Gy照射剂量下,化合物15、16、18、19对人宫颈癌Helo细胞株显示出很好的放射增敏活性,对肿瘤细胞的抑制率达到95%左右。结论金属卟啉结构单元的引入,极大地提高了硝基咪唑类的放射增敏活性。 相似文献
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有机锗倍半氧化物类化合物的合成 总被引:1,自引:0,他引:1
目的:为寻找新型低毒有效放射增敏剂,合成了3 种类型有机锗倍半氧化物。方法:取代桂皮酸或取代苯丙炔酸与三氯锗仿反应,所得加成物经水解即得锗倍半氧化物;三氯锗基丙酰氯与亮氨酸乙酯或苯丙氨酸乙酯反应,所得产物水解即得N-(β-倍半氧锗基 丙酰) 氨基酸酯。结果:合成的8个化合物中,7个(2 ~8) 为新化合物,羧基-β-( 取代苯基)乙烯基锗倍半氧化物为新类型化合物。结论:离体和整体实验结果表明,化合物4 有较显著的放射增敏作用,为新型低毒有效放射增敏剂。 相似文献
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邵建本 《国外医学(药学分册)》1982,(3)
对多种芳香硝基化合物的放射增敏作用研究发现,1-(2-羟基-3-甲氧丙基)-2-硝基味唑(Misonidazole)是一有效的放射增敏剂,但因其神经毒性和诱变性,妨碍其临床应用。为寻找低毒和有效的放射增敏剂,考虑到分子的亲电性的重要作用以及芳环上引入吸电子基可增大活性,合成了一系列2,4-二硝基咪唑衍生物(2~4),并采用中国仓鼠低氧细胞(V-79),进行放射增敏体外试验。 相似文献
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Krishna Challa M Vijaya Bhargavi G L David Krupadanam 《Journal of Asian natural products research》2016,18(12):1158-1168
Taking into consideration of the biological activity of betulinic acid derivatives containing a oxadiazole ring, the semisynthetic betulinic acid-1,2,4-oxadiazole esters (14–25) were synthesized starting from betulinic acid (1) and 5-(bromomethyl)-3-aryl-1,2,4-oxadiazoles (2–13) and final compounds were tested for cytotoxic activity on three human cancer cell lines in vitro. All tested compounds showed good cytotoxic activity. The structures of synthesized compounds are established based on infrared (IR), nuclear magnetic resonance (NMR), and mass spectrometry. 相似文献
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Acylation and Cyclization of N-Hydroxyisoureas by Phenyl Isocyanate On adding phenyl isocyanate to the N-hydroxyisoureas 1 the O-carbamoyl derivatives 4 are obtained. They can undergo ring closure to yield Δ2-1,2,4-oxadiazolin-5-one (5a) , the 3-imino-1,2,4-oxadiazolidin-5-ones 5b–5e or Δ3-1,2,4-oxadiazolin-5-one (9dB) . Compounds 5b–5e form the hydrochlorides 6b–6e which can be hydrolized to yield the 1,2,4-oxadiazolidine-3,5-diones 7b–7e . The IR and MS data of compounds 4–7 are discussed. 相似文献
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L. A. Kayukova K. D. Praliev A. L. Akhelova U. S. Kemel’bekov G. M. Pichkhadze G. S. Mukhamedzhanova D. M. Kadyrova S. R. Nasyrova 《Pharmaceutical Chemistry Journal》2011,45(8):468-471
Three series of amidoxime derivatives including nitrous derivatives of α-chloro-α-isonitrosoacetone and hydrochlorides of
O-aroyl-β-aminopropioamidoximes and 3-[β-(piperidin-1-yl)]ethyl-5-aryl-1,2,4-oxadiazoles were tested for conduction, infiltration,
and terminal anesthesia. There are four interesting “hit” compounds, i.e., the hydrochloride of O-m-chlorophenyl-β-(benzimidazol-1-yl)propioamidoxime (VII), the hydrochloride of O-p-nitrophenyl-β-(benzimidazol-1-yl)propioamidoxime (VIII), 3-[β-(piperidin-1-yl)]ethyl-5-p-tolyl-1,2,4-oxadiazole (IX), and 3-[β-(piperidin-1-yl)]ethyl-5-m-chlorophenyl-1,2,4-oxadiazole (X), which exhibit higher activity than the reference drugs (trimecaine, lidocaine, novocaine, kazcaine). As a whole, all tested
compounds were active in conduction and infiltration anesthesia (at the level of the reference drugs) and did not show activity
in terminal anesthesia. Compounds VII – X are of interest for further testing under condition and infiltration anesthesia conditions. 相似文献
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New 1-[(tetrazol-5-yl)methyl]indole derivatives, their acyclic nucleoside analogs and the corresponding glycoside derivatives
were synthesized. Furthermore, the [)(1,2,4-triazol-3-yl)methyl])-2H-tetrazole derivative as well as the corresponding thioglucoside were prepared. The synthesized compounds were tested for
their antimicrobial activity against Aspergillus Niger, Penicillium sp, Candida albican, Bacillus subtilis, Streptococcus lacti, Escherichia coli, Pseudomonas
sp., and streptomyces sp. Compounds 3, 5 and 19b exhibited potent antibacterial activity and compounds 4, 5 and 10 exhibited high activities against the tested fungi compared with fusidic acid. 相似文献
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A series of novel tricyclic pyrimido[4′,5′:4,5]pyrimido[1,6-a]azepine derivatives were synthesized using the starting compound 3-amino-1-oxo-2-phenyl-5-(pyrrolidin-1-yl)-1,2,4a,5,6,7,8,9-octahydropyrimido[1,6-a]azepine-4-carbonitrile 4. This series includes the 3-aryl derivatives 6a, b, the 3-cycloaminoalkyl derivatives 8a–f, the 3-mercaptomethyl derivatives 10 and 11a, b, the 2-cycloaminomethyl derivatives 13a–c, the 1-cycloamino derivatives 15a–c and the 1-amino derivative 16. The structures of the newly synthesized compounds were elucidated by IR, 1H NMR, 13C NMR, mass spectroscopy and elemental analyses. The anti-inflammatory activity of all newly synthesized compounds was evaluated
using the carrageenan-induced paw oedema test in rats using diclofenac sodium as the reference drug. Ulcer indices for the
most active compounds were calculated. The 3-mercaptomethylacetic acid derivative 10 was the most active compound, showing activity comparable to diclofenac sodium with minimal ulcerogenic effect while the
rest of the tested compound exhibited moderate anti-inflammatory activity. 相似文献
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Alkylation of 3-mercaptophenanthreno[9,10-e]-1,2,4-triazine ( 1b ) yielded the S-alkyl derivatives 2 a-d . Amination of 1a afforded the 3-amino derivatives 3a-h . Reaction of 1a with hydrazine hydrate gave 3-hydrazinophenanthreno[9,10-e]-1,2,4-triazine ( 4 ) which underwent cyclisation with nitrous, formic or acetic acids giving the phenanthreno[9,10-e]-1,2,4-triazino[2,3-d]-1,2,3,4-tetrazole ( 5 ) and the phenanthreno[9,10e]-1,2,4-triazino[2,3-d]-3H-methyl-1,2,4-triazoles 6, 7 . Compound 4 also reacted with methyl [bis(dimethylmercapto)methylene]cyanoacetate, ethyl acetoacetate, ethoxymethylenemalononitrile, ethyl ethoxymethylencyanoacetate or acetyl acetone to yield the 3-(pyrazol-1-yl)-phenanthreno[9,10-e]-1,2,4-triazines 8–12 . 相似文献
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VERONIQUE ISSARTEL PASCAL COUDERT CATHERINE RUBAT SOLANGE NHAMIAS JACQUES COUQUELET 《The Journal of pharmacy and pharmacology》1998,50(6):575-582
A series of 2-(4-arylpiperazin-1-yl-methyl)-4-methyl-1-oxo-5,6,8,8a-tetrahydro-thiazolo[3,4-d] [1,2,4]triazines was prepared and tested for antinociceptive activity. The compounds were prepared by the Mannich reaction from the corresponding 2-unsubstituted thiazolotriazines. When administered intraperitoneally most were found to have potent analgesic activity in the mouse during tests of phenylbenzoquinone-induced abdominal constriction; ED50 values (doses resulting in half the maximum effect) ranged from 10 to 87 mg kg?1. Derivatives with a 3-chloro- or 4-fluorophenylpiperazinylmethyl side-chain in the 2-position of the bicyclic system were, when administered intraperitoneally at doses greater than 25 mg kg?1, also effective in the hot-plate test without associated sedative effects. The compounds have a large therapeutic index; intraperitoneal LD50 values (doses which result in the death of half the animals) were > 700 mg kg?1. Naloxone attenuated the analgesic activity of the 3-chloro derivative, suggesting the participation of μ-receptors in the antinociceptive effects of this drug. In addition, a non-opioid mechanism, probably related to enhancement of the release of 5-hydroxytryptamine and noradrenaline, or inhibition of the neuronal re-uptake of these compounds, has been evinced to explain the analgesic properties of the 3-chloro or 4-fluoro derivatives. These results provide evidence for the involvement of noradrenergic and 5-hydroxytryptaminergic pathways in the analgesic activity of 3 and 4. Because of their potential effectiveness, the 3-chloro- or 4-fluorophenylpiperazinylmethyl derivatives might be suitable for treatment of a wide variety of painful conditions and could be attractive reserve agents for patients dissatisfied with opioids. 相似文献
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Mansour I. Younes Abdel-Alim M. Abdel-Alim Hessan H. Abbas Saoud A. Metwally 《Archiv der Pharmazie》1987,320(12):1196-1202
5-Ethyl-3-hydrazino-5H-1,2,4-triazino|5,6-b|indole ( 2 ) reacts with aromatic aldehydes in anhydrous ethanol to yield substituted arylidene-(5-ethyl-5H-1,2,4-triazino|5,6-b|indol-3-yl)hydrazones 3 . Treatment of 3 with excess SOCl2 gave 10-ethyl-1-aryl-10H-| 1,2,4]triazolo|3′,4′:3,4| 1,2,4|triazino|5,6-b|indoles 4 , while the reaction of 2 with CS2 in methanolic KOH afforded 10-ethyl-2,10-dihydro-1 H-| 1,2,4|triazolo|3′,4′3,4‖ 1,2,4|triazino|5,6-b|indol-1-thione ( 5 ). Fusion of 1 with aromatic amines leads to 3-(arylamino)-5-ethyl-5H-1,2,4-triazino|5,6-b|indoles 6 , whereas the reaction of 1 with alkyl or aralkyl halides in anhydrous acetone and in the presence of anhydrous K2CO3 results in the alkylation of the thiol group to give the alkylthio or aralkylthio derivatives 7. 相似文献
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Daniele Zampieri Maria Grazia Mamolo Erik Laurini Giuditta Scialino Elena Banfi Luciano Vio 《Archiv der Pharmazie》2009,342(12):716-722
2‐Aryl‐3‐(1H‐imidazol‐1‐yl and 1H‐1,2,4‐triazol‐1‐yl)‐1H‐indole derivatives were synthesized and tested for their in‐vitro antifungal and antimycobacterial activities. These indole derivatives were devoid of antifungal activity against the tested strains of Candida spp. Yet, they exhibited an interesting antitubercular activity against Mycobacterium tuberculosis reference strain H37Rv. 相似文献