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1.
在对乙酰乳酸合成酶(AHAS)抑制剂进行生物合理设计的基础上, 分别以4-氟-3硝基苯胺和2-胺基-5硝基苯腈为原料, 合成了8个苯磺酰胺基苯甲酰胺类化合物和7个双苯磺酰胺基苯甲酰胺类化合物, 其结构通过核磁共振谱、质谱、红外光谱及元素分析验证. 初步的生物活性测定结果表明, 部分化合物在体内和体外均具有一定的生物活性, 其中化合物4c, 4d和7c在100 μg/mL浓度下对拟南芥AHAS的抑制率分别为66%, 76% 和68%, 而化合物4a, 4c, 7a和7b在100 μg/mL浓度下对油菜根长的抑制率分别为76%, 70%, 89% 和82%. 研究结果为进一步设计合成潜在的AHAS抑制剂提供了有益参考. 相似文献
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一些吲哚二酮类衍生物的合成及对AHAS的抑制活性 总被引:1,自引:1,他引:0
基于一些新结构特征的AHAS抑制剂, 设计并合成了一系列吲哚二酮类化合物. 初步的生物活性测试结果表明, 所合成的化合物在体内和体外均具有一定的生物活性, 其中, 化合物13在100 μg/mL浓度下对AHAS的抑制达到85%, 化合物7(平皿法)在100 μg/mL浓度条件下对油菜胚根生长抑制率可达84.7%, 是一类未见文献报道的结构新型的AHAS抑制剂, 有望为进一步设计合成更高活性的化合物提供参考. 相似文献
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3位苯甲酰腙和亚氨基取代硫脲取代的吲哚满二酮衍生物的合成及对AHAS的抑制活性 总被引:1,自引:1,他引:0
基于前期生物设计AHAS抑制剂的研究,设计合成了15个吲哚满二酮类衍生物,其中9个为新化合物,其结构均经过1H NMR,MS和元素分析确证,并对所有化合物进行了离体和活体活性测试.实验结果表明,这类化合物在体内和体外均具有一定的生物活性,在离体活性测试中,所有化合物在100μg/mL浓度下对拟南芥AHAS均表现出明确的抑制活性,其中化合物4d,4e,5a和5f在10μg/mL浓度下仍然对AHAS表现出45%以上的抑制率,但此类化合物除草活性普遍较差. 相似文献
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在AHAS与磺酰脲类除草剂复合物的晶体结构基础上, 利用分子对接程序DOCK 4.0, 通过MDL/ACD三维数据库虚拟筛选, 得到了296个与AHAS结合能较低的小分子化合物结构信息, 从中选取了部分小分子进行化学合成, 并且测试了其生物活性. 部分化合物的体内和体外活性表现出一定的一致性. 相似文献
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在前期工作中,含芳硫醚(砜)结构的系列酰胺衍生物在200μg/mL浓度下显示出了优异的杀线虫活性.为了细致研究氟吡菌酰胺中酰胺桥结构修饰对生物活性的影响,通过采取酰胺键翻转、引入N-磺酰基取代的酰胺键,设计、合成了两系列结构新颖的含芳硫醚的酰胺化合物.生物活性测定显示,酰胺桥结构修饰对目标化合物的杀线虫活性和杀菌活性影响较大.其中,相对于化合物Ⅰ,化合物Ⅱ中酰胺键上N-磺酰基的引入有利于改善杀线虫活性.分子对接发现,酰胺桥中羰基或者磺酰基与芳香环直接相连对杀线虫活性是有利的. 相似文献
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用N-取代三氯乙酰胺与3-甲基苯甲酰肼反应,合成了6个新的N-芳基-N'-芳酰基氨基脲.其结构经元素分析、IR和1H NMR证实.生物活性测试结果表明,它们中除2个化合物外均具有一定的除草活性. 相似文献
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3-芳氧基-6-取代哒嗪的合成及其除草活性 总被引:4,自引:0,他引:4
合成了系列3-芳氧基-6-取代哒嗪类化合物.化合物结构经1HNMR、元素分析、IR和MS确证.生物活性测试结果表明,该类化合物具有很好的除草活性,讨论了其结构与除草活性的关系. 相似文献
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Jan Zelenka Dr. Aleksandr Pereverzev Dr. Ullrich Jahn Prof. Dr. Jana Roithová 《Chemistry (Weinheim an der Bergstrasse, Germany)》2022,28(28):e202104493
Photocatalytic generation of nitrenes and radicals can be used to tune or even control their reactivity. Photocatalytic activation of sulfonyl azides leads to the elimination of N2 and the resulting reactive species initiate C−H activations and amide formation reactions. Here, we present reactive radicals that are generated from sulfonyl azides: sulfonyl nitrene radical anion, sulfonyl nitrene and sulfonyl amidyl radical, and test their gas phase reactivity in C−H activation reactions. The sulfonyl nitrene radical anion is the least reactive and its reactivity is governed by the proton coupled electron transfer mechanism. In contrast, sulfonyl nitrene and sulfonyl amidyl radicals react via hydrogen atom transfer pathways. These reactivities and detailed characterization of the radicals with vibrational spectroscopy and with DFT calculations provide information necessary for taking control over the reactivity of these intermediates. 相似文献
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A new and effective procedure is described for the synthesis of N-alkyl and N-aryl 2-F-alkylethylamines avoiding the formation of 2-F-alkylethylethenes usually occuring in the N-alkylation of 2-F-alkylethyl iodides by amines. 相似文献
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Rongxiang Chen Shaohong Xu Fumin Shen Canran Xu Kaikai Wang Zhanyong Wang Lantao Liu 《Molecules (Basel, Switzerland)》2021,26(18)
A simple and rapid method for efficient synthesis of sulfonyl chlorides/bromides from sulfonyl hydrazide with NXS (X = Cl or Br) and late-stage conversion to several other functional groups was described. A variety of nucleophiles could be engaged in this transformation, thus permitting the synthesis of complex sulfonamides and sulfonates. In most cases, these reactions are highly selective, simple, and clean, affording products at excellent yields. 相似文献
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While sulfonyl hydrazides are widely utilized in organic synthesis, it is only in recent years that they have emerged as powerful sulfonyl sources. The hydrazinyl group can be readily removed from sulfonyl hydrazides under thermal, basic, oxidative, radical, and/or transition metal-catalyzed conditions, and subsequently, the remaining sulfonyl groups are able to form carbon-sulfur, sulfur-nitrogen, sulfur-halogen, sulfur-sulfur, and sulfur-selenium bonds with a wide variety of organic compounds, providing alternative approaches to the preparation of sulfones, sulfonamides, sulfonyl halides, thiosulfonates, and selenosulfonates. Moreover, some of the carbon-sulfur bond-forming reactions have been successfully applied to the construction of carbocycles, heterocycles, and stereogenic centers. 相似文献
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Sulfonyl fluoride electrophiles have found significant utility as reactive probes in chemical biology and molecular pharmacology. As warheads they possess the right balance of biocompatibility (including aqueous stability) and protein reactivity. Their functionality is privileged in this regard as they are known to modify not only reactive serines (resulting in their common use as protease inhibitors), but also context-specific threonine, lysine, tyrosine, cysteine and histidine residues. This review describes the application of sulfonyl fluoride probes across various areas of research and explores new approaches that could further enhance the chemical biology toolkit. We believe that sulfonyl fluoride probes will find greater utility in areas such as covalent enzyme inhibition, target identification and validation, and the mapping of enzyme binding sites, substrates and protein–protein interactions. 相似文献
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Seyed Abolghasem Hashemi 《合成通讯》2013,43(24):3352-3356
Stable derivatives of N-alkyl sulfonyl hydrazone were obtained in excellent yields from the reaction between electron-deficient acetylenic ester compounds and sulfonyl hydrazones in the presence of trialkylphosphites in dichloromethan at room temperature. [Supplementary materials are available for this article. Go to the publisher's online edition of Synthetic Communications® for the following free supplemental resource(s): Full experimental and spectral details.] 相似文献
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Nawel Khettache Amel Bendjeddou Malika Berredjem Zine Regainia Veronique Montero Chantal Menut 《合成通讯》2013,43(16):2299-2305
An efficient three‐step synthesis of chiral 1,1′‐(sulfonyl)bisaziridines is described. Preparation of these compounds was carried out easily starting from N,N′‐sulfonyl bis‐(α‐L‐aminoester) to afford the title compounds in very good yields. These 1,1′‐(sulfonyl)bisaziridines can constitute interesting synthetic building blocks. 相似文献
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The ease of preparation and the potential synthetic utility of the N-aryl sulfonyl hydrazimidates is described and the stereochemistry of one of these compounds is unambiguously assigned by X-ray crystallography. 相似文献
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An efficient and operationally simple three-component coupling synthesis of varieties of N-aryl substituted pyrroles is described in the presence of sustainable and environmentally benign metal catalyst, FeCl3. This method provides a straightforward approach for the synthesis of N-aryl substituted pyrroles in good yields from easily accessible starting materials such as nitroalkenes, 1,3-dicarbonyl compounds, and primary aromatic amines. The reaction proceeds through a catalytic sequence of Fe(III)-catalyzed amination/Michael/cycloisomerization reactions. Supplemental materials are available for this article. Go to the publisher's online edition of Synthetic Communications® to view the free supplemental file. 相似文献