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合成并表征了5种4,6-二芳基-2-氨基嘧啶类化合物。 测试了它们对大肠肝菌甲硫酰胺肽酶(EcMetAP)的抑制作用及对CXCR4受体的拮抗作用。 发现5种化合物均对EcMetAP酶活有抑制作用,除化合物2外均对CXCR4受体有拮抗作用。 利用FieldTemplater和FieldAlign软件对化合物1~5的上述活性构效关系进行了分析,初步认为化合物的嘧啶环3位N原子及4位取代苯环上若引入给电子基团,可增强这类化合物的EcMetAP酶抑制活性;在嘧啶环2位引入负电性较强的基团取代,改造2个苯环和嘧啶环的4、5、6位C原子的结构可增强其CXCR4受体拮抗活性。 相似文献
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基于Dl蛋白结构模型,设计并合成了取代苯甲酰胺基丙烯酸乙酯及有关成环化合物嘧啶酮,通过X射线衍射确定了2-芳基-5-乙氧甲酰基-6-甲硫基-4-嘧啶酮的结构.生物活性测定结果表明,部分化合物显示出一定的Hill反应抑制活性. 相似文献
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基于Dl蛋白结构模型,设计并合成了取代苯甲酰胺基丙烯酸乙酯及有关成环化合物嘧啶酮,通过X射线衍射确定了2-芳基-5-乙氧甲酰基-6-甲硫基-4-嘧啶酮的结构.生物活性测定结果表明,部分化合物显示出一定的Hill反应抑制活性. 相似文献
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以2,4-二氯嘧啶为起始物设计并合成了一系列4-芳(硫)氧基-2-氯嘧啶和4-芳氧基-2-二甲氨基嘧啶化合物。利用2,4-二氯嘧啶2个氯原子的活性差异,酚取代嘧啶环上4位氯原子,然后二甲氨基取代2位的氯原子。所合成的化合物均经过了1H NMR和元素分析确证。为了确证酚首先在嘧啶环的4位发生亲核取代反应,用X衍射法测定了化合物3d的单晶结构。初步生物活性测定结果表明,大部分化合物都表现出一定的除草活性,其中化合物7c、7j、7k和7m在1.0×10-4g/mL质量浓度下对油菜的抑制率达到了80%以上。 相似文献
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嘌呤、嘧啶类新手性化合物的合成 总被引:25,自引:0,他引:25
把具有生理活性的嘌呤、嘧啶类有机碱基引入不对称合成 ,利用嘌呤、嘧啶类化合物作为Michael加成给体与天然手性助剂 ( - ) 薄荷醇所制得的手性源 5 (R) [( 1R ,2S ,5R) 氧基 ] 2 ( 5H) 呋喃酮 ( 3a)进行不对称Michael加成反应 ,合成了新的光学纯嘌呤、嘧啶类手性化合物 ( 5a~ 5e) .详细地研究了合成方法并测定了它们的[α],IR ,UV ,1HNMR ,13 CNMR ,MS ,元素分析等结构分析数据 .经X 四圆衍射确定了腺嘌呤手性化合物 5a的立体化学结构 .为合成嘌呤、嘧啶类手性化合物提供了有效的途径 ,为深入研究具有生理活性的手性核苷酸类化合物提供了重要的手性源 相似文献
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5,7-二甲基-1,2,4-三唑并[1,5-a]嘧啶-2-氧乙酰腙类衍生物的合成与生物活性 总被引:18,自引:0,他引:18
以5,7-二甲基-1,2,4-三唑并[1,5-a]嘧啶-2-甲硫醚为起始原料, 设计合成了15个新型的5,7-二甲基-1,2,4-三唑并[1,5-a]嘧啶-2-氧乙酰腙及10个(R)-5,7-二甲基-1,2,4-三唑并[1,5-a]嘧啶-2-氧(α-甲基)乙酰腙类化合物, 通过元素分析、 MS和 1H NMR对所合成的化合物进行了结构表征. 初步生物活性测试结果表明, 部分化合物表现出不同程度的除草及杀菌活性. 目标化合物中引入手性中心有利于生物活性的提高. 相似文献
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嘧啶环是生物活性化合物中具有较好生理活性的基因。本文试图将嘧啶环引入农用药剂,合成系列酰胺类化合物。生物试验结果表明,其中一些化合物具有杀蝇效能,一些化合物对较难防治的寄生疫霉具有良好的抑制效能。 相似文献
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Phenyltriazolinones are one of the most important classes of herbicides targeting the protoporphyrinogen oxidase enzyme. A series of triazolinone derivatives containing a strobilurin pharmacophore were designed and synthesized with the aim of discovering new phenyltriazolinone analogues with high activity. The herbicidal activity of the synthesized compounds was assayed and some of the test compounds displayed moderate herbicidal activity at 150 g ai/ha. 相似文献
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Barbara Lejczak Jan Zygmunt Roman Gancarz Roman Tyka Paweł Kafarski Lucyna Koba 《Phosphorus, sulfur, and silicon and the related elements》2013,188(1-4)
Abstract Over 40 phosphonic, phosphinic and phosphinous acid analogues of phenylglycine and phenylalanine were synthesized and screened for their herbicidal activity on Lepidium sativum (crest) and Cucumis sativus (cucumber). The most active appeared to be 2-amino-1-hydroxy-3-phenylpropylphosphonic acid which was equipotent with popular herbicide glyphosate. Also aminobenzylphosphonic acids, analogues of phenylglycine, exhibited notable herbicidal activity and thus represent a group of the most active herbicides found among simple aminophosphonic acids. Other compounds showed moderate herbicidal activity. Preliminary results indicate that analogues of aromatic amino acids display their activity as effectors of biosynthesis of aromatic amino acids. 相似文献
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《Journal of heterocyclic chemistry》2017,54(1):670-676
Using 3‐(4‐cyano phenoxy)‐6‐methyl‐4‐(3‐trifluoromethylphenyl) pyridazine (compound A ) as a leading compound, a total of 24 novel 3‐(substituted phenoxy)‐6‐methyl‐4‐(3‐trifluoromethylphenyl) pyridazine derivatives containing two electron‐withdrawing groups on the benzene ring (acylamine and oxime ether) were synthesized. Their herbicidal, insecticidal activities were bioassayed, and the herbicidal activity of compound CD-2 against Brassica campestris was 97.6% at 300 g/ha, which was better than the commercial herbicide diflufenican at the this concentration and is equal to the activity of the leading compound A . Compound CD-4 , CD-5 , CJ-3 , and CJ-5 displayed excellent insecticidal activity against Aphis laburni Kaltenbach (>95%). The results show that the oxime ether substitutions exhibit better bleaching and herbicidal activity than the acylamine ones. The bleaching and herbicidal activity of para‐position substitutions is better than the meta‐position ones. It seems that the para‐position on the benzene ring of oxime ether pyridazine derivatives is one of the key active sites that affect their herbicidal activities. 相似文献
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Ting Chen Ping Shen Yanjun Li Hongwu He 《Phosphorus, sulfur, and silicon and the related elements》2013,188(9):2135-2145
To investigate the influence of a fluorine moiety on the biological activity of phenoxyacetoxyalkylphosphonates, a series of fluorine-containing phenoxyacetoxyalkylphosphonates were synthesized and screened for herbicidal activity in a greenhouse. The majority of the title compounds showed better preemergence activity than postemergence activity against the test plants, especially on monocotyledon. Compound 5l exhibited notable activity. Results showed that by introducing a fluorine moiety to the parent structure of phenoxyacetoxyalkylphosphonates, a series of new compounds with satisfactory herbicidal activity could be synthesized. A reasonable combination of a fluorine moiety and other substituents on the benzene ring had a great influence on the herbicidal activity. 相似文献
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Synthesis and herbicidal activity of O,O-dialkyl phenoxyacetoxyalkylphosphonates containing fluorine
Ting Chen 《Journal of fluorine chemistry》2006,127(2):291-295
A series of substituted phenoxyacetoxyalkylphosphonates bearing fluorine were designed and synthesized. All the new compounds were identified by elemental analysis, IR, 1H NMR and MS and were tested for herbicidal activity in greenhouse at a rate of 1.5 kg/ha. The results of preliminary bioassay showed that fluorine moiety introduced to the core structure could help to improve the herbicidal activity, and compounds with a 3-trifluoromethyl in benzene ring exhibited higher inhibitory activity. 相似文献
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2H-1,2,4-噻二唑并[2,3-a]嘧啶衍生物的合成及除草活性研究(Ⅲ) 总被引:2,自引:3,他引:2
合成了10个新的2-乙氧甲酰亚胺基-2H-1,2,4-噻二唑并[2,3,-a]嘧啶类化 合物,结构经IR,^1H NMR,MS和元素分析确证,除草活性测定结果表明,部分目标 化合物具有良好的除草性且选择性较好,对双子叶植物安全。 相似文献
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以ALS为靶标的新型除草剂的分子设计、合成及生物活性研究(Ⅵ)——嘧啶(硫)醚类除草剂的电子结构研究及新型除草剂的分子设计 总被引:6,自引:0,他引:6
从量子药理学的角度,对嘧啶(硫)醚类化合物的电子结构进行了量子化学研究.结果表明,在高活性分子的嘧啶环周围存在一个大的电负性区域,其除草活性与杂环部分的电荷转移能力有关.在上述结果的基础上,设计并合成了一类结构新颖的除草剂.生测结果表明,所设计的化合物具有很好的除草活性,其中化合物b的pIC50达到7以上. 相似文献
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R. Bacardit J. Cervell P. de March J. Marquet M. Moreno-Maas J. L. Roca 《Journal of heterocyclic chemistry》1989,26(5):1205-1212
New derivatives of dehydroacetic acid and triacetic acid lactone functionalized at both C-5 and at the methyl group at C-6 have been synthesized as intermediates for the preparation of thromboxane B2 analogues. 6-Mercaptomethyl-4-methoxy-2-pyrone and some derived thioethers have been also prepared. New thioether derivatives of O-alkyloximes of dehydroacetic acid have been synthesized and tested for herbicidal activity. 相似文献
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以昆虫乙酰胆碱受体为作用靶标的新烟碱类杀虫剂属于高效、高选择性和环境友好的杀虫剂,依据新烟碱类杀虫剂活性与结构关系,以吡虫啉及其类似物NTN32692为先导结构,在咪唑啉环位置并入可以增强分子脂溶性的六元环基团,设计合成了9个未见文献报道的硝基亚甲基类新烟碱化合物,所有目标化合物的结构均经1H NMR、IR和HR-MS测试技术的确证。初步的生物活性测试结果表明,在500 mg/L下所有目标化合物对豆蚜(Aphis craccivora)都有一定的杀死活性,其中活性最高的化合物4对豆蚜(Aphis craccivora)的校正死亡率为73.0%。并对目标化合物5a~5h的合成方法进行了探讨。 相似文献