共查询到18条相似文献,搜索用时 119 毫秒
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球虫病是家禽养殖业中最常见的寄生虫病之一,目前对该疾病最有效的防治手段是化学药物防治。伴随着现有药物纷纷由于耐药性而出现的疗效降低,开发新的抗球虫药物迫在眉睫。本文以邻苯基苯酚作为起始原料合成了一系列6-苄氧基-7-苯基-4-羟基喹啉-3-羧酸乙酯化合物,并利用~1H NMR,~(13)C NMR,和HR-MS等分析测试方法对化合物结构进行了表征,最后采用抗球虫指数(ACI)方法对目标化合物进行了生物活性测试,测试结果表明化合物5a和5f具有明显的抗球虫效果。 相似文献
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在K2CO3作为碱、乙腈作为溶剂的条件下,将2-氯甲基-4-苯基喹啉-3-羧酸乙酯(3)分别与5,7-二氯-8-羟基喹啉(4a)和5,7-二溴-8-羟基喹啉(4b)发生Williamson反应,以高收率得到结构新颖的二氯或二溴取代的双喹啉类目标化合物2-(5,7-二氯/二溴-8-喹啉氧甲基)-4-苯基喹啉-3-羧酸乙酯(2a,2b);其结构经波谱数据和元素分析证实. 相似文献
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6-氨基-2-取代吲哚-3-羧酸乙酯及其衍生物的合成与生物活性评价 总被引:4,自引:0,他引:4
以2,4-二硝基氯苯和乙酰乙酸乙酯为原料, 经过亲核置换、还原-环化协同反应, 合成了6-氨基-2-甲基吲哚-3-羧酸乙酯, 而后在催化剂作用下, 与乙酰乙酸乙酯反应生成烯胺, 环化合成9-羟基-2,7-二甲基吡咯(2,3-f)喹啉-3-羧酸乙酯; 类似地, 合成了6-氨基-2-苯基吲哚-3-羧酸乙酯和6-氨基-2-(呋喃-2'-基)吲哚-3-羧酸乙酯. 其结构均由1H NMR, IR以及MS波谱数据表征. 所得化合物具有抑制肺癌A549细胞生长的活性, 其抑制效果具有浓度依赖性. 相似文献
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Kisil' S. P. Burgart Ya. V. Saloutin V. I. 《Russian Journal of Organic Chemistry》2001,37(10):1455-1462
For the first time were obtained ethyl 2-(2-methoxy-3,4,5,6-tetrafluorobenzoyl)-3-oxobutanoate and ethyl 2-pentafluorobenzoyl-3-oxobutanoate and their copper chelates. The compounds were prepared by acylation of ethyl acetoacetate with 2-methoxy-3,4,5,6-tetrafluoro- and pentafluorobenzoyl chlorides. Cyclization of these ,'-dioxoesters afforded substituted chromones. 2-Methyl-5-methoxy-6,7,8-trifluoro-3-ethoxycarbonylchromone hydrolyzes depending on reaction conditions either to 5-hydroxy-2-methyl-6,7,8-trifluorochromone or to 5-hydroxy-2-methyl-6,7,8-trifluorochromone-3-carboxylic acid. Reaction with morpholine provided 7-substituted product, and with aqueous ammonia as a result of rearrangement forms 3-acetimidoyl-4-hydroxy-5-methoxy-6,7,8-trifluorocoumarin. Hydrolysis of the latter yields 3-acetyl-4-hydroxy-5-methoxy-6,7,8-trifluorocoumarin. 相似文献
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Yuan Yuan Zhang Xing Yan Zeng Kui Nie Zhi Cheng Zhong Yu Liang Wang Yu Zhong Wang 《中国化学快报》2010,21(4):426-428
<正>A series of ethyl 6-alkoxy-7-phenyl-4-hydroxy-3-quinolinecarboxylates were designed and synthesized.Their structures were confirmed by ~1H NMR,~(13)C NMR,IR and HRMS.The biological activities were primarily evaluated against Eimeria tenella according to Anticoccidial Index(ACI) method in vivo.The results showed that compounds 5e,5f and 5i exhibited anticoccidial activities against E.tenella at 27 mg kg~(-1). 相似文献
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B. V. Lichitskii A. O. Osipov A. N. Komogortsev A. A. Dudinov M. M. Krayushkin 《Russian Chemical Bulletin》2014,63(2):457-461
A convenient method for the synthesis of earlier unknown substituted derivatives of 4-aryl-7-methyl-4,6-dihydro-3H-pyrano[3,2-c]pyridine-2,5-dione and ethyl 3-(4-hydroxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)-3-arylpropionate was developed based on the multi-component condensation of 4-hydroxy-6-methyl-1H-pyridin-2-one, Meldrum’s acid, and carbonyl compounds. 相似文献
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The synthesis of 1,4-dihydro-1-methoxy or ethyl -2-methyl-4-oxo-3-quinolineglyoxylic acid derivatives are described. α-Acetoxy-1,4-dihydro-1-hydroxy-2-methyl-4-oxo-3-quinolineacetic acid esters ( 7a, 7a ), which are key intermediates, were prepared by catalytic hydrogenation of 2-acetoxy-3-acetyl-4-hydroxy-4-(2-nitrophenyl) crotonic acid lactone ( 6 ) in methanol or ethanol. 相似文献
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ZHAO Chun-shen ZHAO Yan-fang CHAI Hui-fang GONG PingLiaoning Province Key Laboratory of Innovative Medicine Research Design Shenyang Pharmaceutical University Shenyang P. R. China 《高等学校化学研究》2006,22(5)
IntroductionHepatitis B caused by a virus(HBV)is a commoninfectious disease in the world.According to WHO,700million people have been infected with HBVin theworld[1,2].HBV infection causes severe liver diseasesuch as cirrhosis and may also eventually lead… 相似文献
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Isothiazolopyridines, pyridothiazines and pyridothiazepines are important compounds that possess valuable biological activities. This paper reports on the synthesis of these compounds using both conventional chemical methods and modern microwave techniques. 3-Bromo-6-hydroxy-4-methyl-2-thioxo-2,3-dihydropyridine-3-carboxamide, 5-arylazo-6-hydroxy-4-methyl-2-thioxo-1,2-dihydropyridine-3-carboxamides, 3,5-bis-arylazo-6-hydroxy-4-methyl-2-thioxo-2,3-dihydropyridine-3-caboxamide, 4-methyl-2,3,6,7-tetra-hydroisothiazolo[5,4-b]-pyridine-3,6-dione, 2,2'-(methylene-bis-(sulfanediyl))bis(4-methyl-6-oxo-1,6-dihydropyridine-3-carboxamide), 2-hydroxy-5-methyl-4H-pyrido[3,2-e][1,3]-thiazine-4,7(8H)-dione and 2-arylmethylene-8-hydroxy-6-methyl-2,3,4,5-tetrahydropyrido-[3,2-f][1,4]thiazepine-3,5-diones have been prepared from 6-hydroxy-4-methyl-2-thioxo-2,3-dihydropyridine-3-carboxamide. Some of these compounds were prepared using microwave-assisted reaction conditions, that provided higher yields in shorter times than the conventional methods. 相似文献
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M. Mercedes Blanco Isabel A. Perillo Celia B. Schapira 《Journal of heterocyclic chemistry》1999,36(4):979-984
A number of 8-hydroxy-6-methyl-1,6-naphthyridin-5(6H)-one-7-carboxylic acid alkyl esters 3 and the isomeric 5-hydroxy-7-methyl-1,7-naphthyridin-8(7H)-one-6-carboxylic acid alkyl esters 4 were synthesized from acyclic precursors obtained starting from quinolinic anhydride 5. Thus, methanolysis of 5 afforded the hemiester 6 which treated with oxalyl chloride and sarcosine ethyl ester gave 3-(N-ethoxycarbonylmethyl-N-methylcarbamoyl)pyridine-2-carboxylic acid methyl ester 8. Compound 8 was cyclized to naphthyridines 3a-e with sodium alkoxides. The isomeric naphthyridines 4a-c were obtained by cyclization of the open intermediary 2-(N-ethoxycarbonylmethyl-N-methylcarbamoyl)pyridine-3-carboxylic acid methyl ester 9 obtained by a route that involves treatment of 5 with sarcosine ethyl ester and esterification with diazomethane. Spectroscopic properties (1H nmr, uv, ir) of compounds 3 and 4 are discussed and confirmed the proposed structures. 相似文献
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Seo Y Park KE Kim YA Lee HJ Yoo JS Ahn JW Lee BJ 《Chemical & pharmaceutical bulletin》2006,54(12):1730-1733
Thunbergols A (4) and B (5), tetraprenyltoluquinols, along with three known compounds (1-3) have been isolated from the brown alga Sargassum thunbergii. The structures of these two new compounds were determined to be 9-(3,4-dihydro-2,8-dimethyl-6-hydroxy-2H-1-benzopyran-2-yl)-6-methyl-2-(4-methyl-3-pentenyl)-(2E,6E)-nonadienoic acid (4) and 10-(2,3-dihydro-5-hydroxy-7-methyl-1-benzofuran-2-yl)-10-hydroxy-6-methyl-2-(4-methyl-3-pentenyl)-(2E,6E)-undecadienoic acid (5), respectively, by combined spectroscopic methods. Both of them exhibited significant scavenging activities on radical and potently inhibited generation of ONOO(-) from morpholinosydnonimine (SIN-1). 相似文献