共查询到19条相似文献,搜索用时 250 毫秒
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β-内酰胺类抗生素是目前最具应用价值的抗生素, 其结构特征具有β-内酰胺环的基元结构, 该类化合物的设计、合成和立体化学研究一直是有机合成化学研究的前沿和热点领域. 二茂铁凭借其独特的结构和多样的性质, 在生物和医药方面均有广泛的应用价值. 因此, 二茂铁修饰的β-内酰胺是一类结构新颖且具有潜在生物活性的化合物. 对该类化合物的深入研究, 将对新型抗生素的研发提供重要的指导意义. 综述了近年来青霉烷类和头孢烯类β-内酰胺及单环类β-内酰胺这两大类含二茂铁取代的β-内酰胺衍生物的合成与生物活性的研究进展. 相似文献
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在无水无氧、超声辐射下, N-取代苄基脯氨酸苄基酯与取代苯基溴化镁反应合成了7个未见文献报道的N-苄 基-α,α-二苯基-2-吡咯烷甲醇衍生物, 其结构经IR, 1H NMR和元素分析测试确证, 并且初步生物活性测定结果表明目标化合物均有较好的杀虫活性. 相似文献
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O,O'-二烷基-α-(取代苯并噻唑-2-基)氨基-(取代苯基甲基)膦酸酯的合成与抗烟草花叶病毒活性 总被引:1,自引:0,他引:1
采用无溶剂无催化剂合成方法, 分别进行了以O,O'-二烷基亚磷酸酯、3,4,5-三甲氧基苯甲醛、2-氨基取代苯并噻唑为原料的类Mannich一锅法合成反应研究, 经合成筛选, 优选出控制反应温度100 ℃, 无溶剂、无催化剂加热反应120 min的合成方法, 实验结果表明该方法经济、简便、对环境友好. 经元素分析, IR, 1H NMR, 13C NMR对所合成的化合物进行了结构确认和表征. 培养并测定了化合物4a的晶体结构. 初步生物活性测试表明, 化合物具有一定的抗烟草花叶病毒活性. 相似文献
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新型手性<i>β</i>-烷氨基-<i>γ</i>-(<i>l</i>-孟氧基)丁内酯的合成 总被引:1,自引:0,他引:1
脂肪族伯胺作为亲核试剂与手性合成子5(R)-(l-孟氧基)-2(5H)-呋喃酮(4)发生不对称Michael加成反应, 得到一系列新的手性β-烷氨基-γ-(l-孟氧基)丁内酯类化合物6(产率34~81%, de≥98%). 通过IR, 1H NMR, 13C NMR, MS, 元素分析及单晶X射线衍射分析, 确认了它们的化学结构、立体化学和绝对构型. 此结果为某些具有生物活性化合物及复杂分子的合成提供了新的途径. 相似文献
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合成了双客体化合物N,N'-双二茂铁亚甲基丁二胺的季铵盐(1)和侧链携带β-环糊精(β-CD)的聚丙烯酰胺(3), 利用FTIR, 1H NMR, 元素分析等手段表征了合成化合物. 在此基础上以1H NMR、循环伏安、X射线粉末衍射以及扫描电镜等手段研究了化合物1与3间的主客体包结作用. 结果表明, 处于1两端的二茂铁基均可被位于3侧链的β-CD包结, 引起高分子化合物3分子内和分子间的物理交联, 形成超分子三维网络结构. 相似文献
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含氟β-氨基酸及其衍生物具有特殊的生理活性, 其合成方法的研究近年来受到广泛关注. 以直接氟化法和间接氟化法分类, 概述了含氟β-氨基酸及其衍生物的合成方法及最新研究进展, 对一些已知化合物的生理活性及药用价值作了初步归纳. 相似文献
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为了寻找新型高效低毒的抗糖尿病分子,由Mannich反应一步合成了15个新的含有异噁唑结构单元的β-氨基酮,制备方法简便、反应条件温和、产品易纯化,收率为51.2%~89.3%.所得化合物结构均通过1HNMR,13CNMR,ESIMS和HRMS表征.生物活性实验结果表明,在低浓度范围,目标分子对蛋白质酪氨酸磷酸酶1B和α-葡萄糖苷酶抑制活性不高,但对过氧化物酶体增殖物激活受体的激动活性强度中等,其中化合物1-(3,4-二氯苯基)-3-(5-甲基异噁唑-3-氨基)-3-(6-甲氧基萘-2-基)-1-丙酮(15)的过氧化物酶体增殖因子活化受体(PPAR)激动活性最好,达到75.3%,值得进一步研究.还讨论了目标分子的合成条件及其结构-活性关系. 相似文献
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Synthesis,Dissociation Constants,and Antimicrobial Activity of Novel 2,3‐Disubstituted‐1,3‐thiazolidin‐4‐one Derivatives 下载免费PDF全文
Łukasz Popiołek Joanna Stefańska Małgorzata Kiełczykowska Irena Musik Anna Biernasiuk Anna Malm Monika Wujec 《Journal of heterocyclic chemistry》2016,53(2):393-402
In this article, a new series of 2,3‐disubstituted‐1,3‐thiazolidin‐4‐one derivatives have been designed, synthesized, and evaluated as antimicrobial agents. New compounds were prepared by the cyclization reaction of N‐substituted carboxylic acid hydrazide derivatives with mercaptoacetic acid. The structures of the obtained compounds were confirmed by means of IR, 1H NMR, and 13C NMR spectra. The dissociation constants were determined using spectrophotometric method. All synthesized compounds were tested for their in vitro antibacterial and antifungal activities using the broth microdilution method. 相似文献
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Isabel Iriepa F. Javier Villasante Enrique Gálvez Antonio Herrera Angel Sánchez Felix H. Cano 《Central European Journal of Chemistry》2005,3(4):683-704
This paper synthesizes N-substituted phthalimides derived from nitrogen heterocycles as potential 5-HT4 ligands by using the Mitsunobu reaction. Conformational studies of some of the new compounds have been conducted using 1H and 13C-NMR spectroscopy. Proton and carbon resonances were achieved through the application of one-dimensional selective NOE, two-dimensional
NMR techniques-homonuclear COSY-45, NOESY and heteronuclear 1H-13C HMQC correlated spectroscopy- and double resonance experiments. The crystal structure of compound 1 was determined by X-ray diffraction. 相似文献
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Naki Çolak Yılmaz Yıldırır Mustafa Kavutcu Nilhan Nurlu 《Monatshefte für Chemie / Chemical Monthly》2007,138(12):1283-1287
Summary. Methotrexate (MTX) is a folate antagonist used in treatment of several chronic inflammatory and neoplastic conditions. In this study, new MTX-like compounds that may-be potential anticancer agents were synthesized and their structures were determined by IR, UV, GC-MS,
1H NMR, and 13C NMR spectra. Also, in this study, a series structurally related to MTX or folate analogous compounds were evaluated whether they have inhibitory properties on the dihydrofolate reductase activity
(DHFR). 相似文献
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Jian‐Nan Xiang Li‐Hui Jiang Chao‐Yue Chen Zhi‐ying Fu Jun‐Fei Duan Xiao‐Xiao He 《Journal of carbohydrate chemistry》2013,32(7):595-614
New retinoyl sugar derivatives of 13‐cis‐retinoic acid were synthesized in three ways in this paper in order to enhance pharmacal effects, especially antiproliferative activities of 13‐cis‐retinoic acid. Their structures were confirmed by IR, 1H‐NMR, 13C‐NMR, and MS spectra and their antiproliferative activities were determined in vitro using human cancer lines. Results showed that some compounds possessed potential antitumor activities. 相似文献
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《Journal of heterocyclic chemistry》2018,55(5):1189-1192
A new class of substituted 2‐amino‐4‐(2‐ethoxybenzo[d][1,3]dioxol‐5‐yl)‐4H‐pyran‐3‐carbonitrile derivatives catalyzed by Imidazole under mild reaction conditions has been developed. A variety of functionalized 2‐amino‐4‐(2‐ethoxybenzo[d][1,3]dioxol‐5‐yl)‐4H‐pyran‐3‐carbonitrile scaffolds were assembled in high yields by this catalytic protocol. The newly synthesized compounds have been characterized by IR, 1H NMR, 13C NMR, and mass spectral data. The compounds were then evaluated for antimicrobial activities. 相似文献
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Hua Fang Weizhu Chen Bihong Hong Yufen Zhao Meijuan Fang 《Phosphorus, sulfur, and silicon and the related elements》2013,188(11):2182-2193
This article describes the synthesis of α-hydroxyphosphonic acid esters using the Pudovik reaction. IR, 1H NMR, 13C NMR, 31P NMR, MS, and elemental analysis were employed to confirm their structures. X-ray structure analysis is reported for six compounds. The antibacterial activities of these compounds are also reported. 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. 相似文献