3-芳亚甲基联氨羰基-5-(对位取代苯基)-吡唑衍生物的 合成、结构和生物活性

以4-取代苯乙酮及草酸二乙酯为起始原料, 设计合成了20个新的3-芳亚甲基联氨羰基-5-(对位取代苯基)-吡唑衍生物, 产率较高. 所合成的化合物经元素分析, IR, 1H NMR对其结构进行了表征, 化合物4b, 4h还通过X-ray单晶衍射进一步确证了其结构. 初步生物活性实验结果表明, 所合成的化合物对绿豆发芽过程有着较好的生长调节作用.     

含氯羧酸吡唑醛肟酯化合物的合成及生物活性

含氯羧酸吡唑醛肟酯化合物的合成及生物活性;羧酸吡唑醛肟酯;合成;生物活性     

含嘧啶环的苯基磺酰脲、吡唑磺酰脲的合成及生物活性

磺酰脲衍生物;除草活性;含嘧啶环的苯基磺酰脲、吡唑磺酰脲的合成及生物活性     

新型含噻唑环的吡唑肟醚类衍生物的合成及其生物活性

为了寻找活性较好的杂环农药,将噻唑基团引入到吡唑分子结构中,设计合成了一系列新型含噻唑环的吡唑肟醚衍生物.通过1H NMR、13C NMR和元素分析测试对标题化合物的结构进行了表征.对合成的目标化合物进行了初步的生物活性测试,部分化合物显示出一定的的杀菌、杀虫或植物生长调节活性.     

取代吡唑啉衍生物的合成与生物活性

采用α-三唑-β-烷氧基芳酮与肼关环,制备了1,3-二苯基-4-三唑基吡唑啉1a,1-苯基-3-对氯苯基-4-三唑基吡唑啉1b和3-取代苯基-4-三唑基吡唑啉(7),并研究了化合物7的成环优化条件.使用α,β-不饱和酮与肼关环合成了1,3,4,5-多取代吡唑啉衍生物1c-1h,并初步用质谱法确定了该反应产物的结构;同时,以3,5-二取代吡唑啉(6)和7作为中间体合成了1-,3-,4-或5-取代的化合物2a-2l.初步生物活性测定结果表明,所合成的化合物均有一定的杀菌、激素和除草效果.     

含哌嗪的吡唑酰胺衍生物的合成与生物活性

设计合成了16个新型的含哌嗪的吡唑酰胺衍生物,所有化合物结构经1 H NMR、13C NMR、IR和元素分析表征.初步生物活性测试表明,在试验浓度下,部分目标化合物表现出一定的抗菌活性和较好的抗TMV活性.     

吡唑类化合物的合成研究进展

吡唑类化合物是一类重要的药物合成中间体,在抗肿瘤、抗病毒、抗抑郁等领域发挥着重要作用。本文综述了吡唑类衍生物的合成方法,包括1,3-亲电化合物与肼类的环化、1,3-偶极体系的环加成等。     

1-苯基-3-甲基-5-芳氧基-1H-吡唑-4-甲醛-O-[(2-氯吡啶-5-基)甲基]肟的合成与生物活性

利用1-苯基-3-甲基-5-芳氧基吡唑4-甲醛肟与2-氯-5-氯甲基吡啶发生缩合反应,合成了14个新型含吡啶环的吡唑肟醚衍生物.通过1H NMR,13C NMR和元素分析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,在试验浓度下部分化合物具有一定的杀菌和植物生长调节活性.     

1-(取代吡唑-4-甲酰基)吡唑类化合物的合成及生物活性研究

设计合成了25个新型1-取代吡唑甲酰基吡唑系列衍生物,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,该类化合物具有一定除草活性,讨论了其结构与活性的关系.     

吡唑衍生物的合成及生物活性

以５－吡唑甲酰肼（７，８）为原料合成了４类共３０种新化合物，这些化合物的结构均经＾１Ｈ ＮＭＲ，元素分析证实，部分化合物还经过了ＭＳ、ＩＲ确证，对大部分化合物做了生物活性测试，结果表明均具有一定的杀菌和除草活性。     

N-(2-(腈基(4,6-二甲氧基嘧啶-2-基)甲基)苯基)酰胺类衍生物的合成及生物活性

以2-(2-硝基苯基)乙腈及4,6-二甲氧基-2-甲磺酰基嘧啶为起始原料,分别经缩合、还原及酰胺化反应合成了6个未见文献报道的N-(2-(腈基(4,6-二甲氧基嘧啶-2-基)甲基)苯基)酰胺类衍生物,其结构经1H NMR、MS和元素分析进行了确证。 在150 g/hm2的用量条件下,合成化合物未显示出除草活性。 在200 mg/L浓度下,部分化合物对黄瓜灰霉病及水稻纹枯病表现出一定的抑菌作用,其中化合物4d对水稻纹枯病的抑制率为72.33%。     

阿魏酸酰腙类化合物的合成及生物活性

将酰腙结构引入到阿魏酸衍生物中,合成了6个阿魏酸酰腙类化合物,其结构经过了IR、~1H NMR、~(13)C NMR和ESI-HRMS表征。抗病毒活性测试结果表明,在质量浓度为500mg/L时,化合物3、5和6对烟草花叶病毒(TMV)在保护、治疗和钝化活性方面的抑制率均优于对照药剂病毒唑。进一步的EC_(50)测试结果表明,化合物3、5和6钝化活性的EC_(50)值分别为91.25、54.86、58.22mg/L,明显低于病毒唑的EC_(50)值(126.05mg/L)。该研究结果表明,阿魏酸酰腙类化合物对TMV具有较好的抗病毒活性,对其进行适当的结构改进和优化,有望得到具有更高抗病毒活性的化合物。     

取代噻吩双酰胺类化合物的设计、 合成及生物活性

利用中间体衍生化方法, 将噻吩环引入到双酰胺类化合物中, 合成了一系列取代噻吩双酰胺类化合物1~3; 目标化合物的结构经核磁共振波谱、 红外光谱及元素分析确认. 生物活性测试结果表明, 化合物1在600 mg/L剂量下对小菜蛾具有良好的杀虫效果, 致死率均为100%, 其中化合物1a和1e在20 mg/L剂量下对小菜蛾的致死率仍达到60%以上; 改变双酰胺结构中的吡唑环得到化合物2和3, 其杀虫活性消失, 说明该类化合物中吡唑环结构对杀虫活性具有关键作用.     

2-取代酰氨基-5-去氢枞基-1,3,4-噻二唑衍生物的合成及杀菌活性

为了寻找具有更高生物活性的新颖先导化合物,本文以去氢枞酸为原料,设计并合成了11个具有1,3,4-噻二唑骨架的新型去氢枞酸衍生物,通过1H NMR、13C NMR、IR、EI-MS和元素分析确认了目标产物的结构。初步的生物活性测试结果表明,大部分化合物具有一定的杀菌活性,其中,化合物2在浓度为50mg/L时对番茄早疫病菌的抑制率达88.9%。     

新型双杂环修饰的酰胺硫醚衍生物的合成和生物活性

首次设计并合成了16个新型1,2,4-三唑与1,3,4-噻二唑双杂环修饰的酰胺硫醚衍生物,并对其进行了结构表征。分别评价了目标分子对蛋白酪氨酸磷酸酶1B(PTP1B)和细胞分裂周期25磷酸酶B(Cdc25B)抑制活性,结果发现:16个目标分子对PTP1B具有良好的抑制活性,其中8-C-d和8-D-c的抑制作用最佳,半抑制浓度(IC_(50)值)分别为(1.19±0.22)mg/L和(1.08±0.09)mg/L,优于阳性参照物齐墩果酸(IC_(50)=(1.27±0.19)mg/L),有望作为抗糖尿病药物先导物;对Cdc25B抑制活性测试中,11个目标分子表现出良好的活性,其中8-A-d、8-C-d和8-D-c抑制活性的IC_(50)值分别为(0.97±0.05)、(1.06±0.03)和(0.94±0.11)mg/L,低于阳性参照物Na_3VO_4(IC_(50)=(1.25±0.14)mg/L),有望作为抗肿瘤药物先导物。     

Synthesis and biological activity of novel N-(3-furan-2-yl-1-phenyl-1H-pyrazol-5-yl) amides derivatives

A series of novel N-(3-furan-2-yl-1-phenyl-1H-pyrazol-5-yl) amides derivatives were designed and synthesized. Their structures were confirmed by ¹H NMR, ¹³C NMR and HRMS. All title compounds were evaluated for their herbicidal and antifungal activities. Preliminary bioassay results indicated that the title compounds showed good to moderate herbicidal activity at 1000 mg/L. Compound 6q presented the best activity against Digitaria sanguinalis (L) Scop., Amaranthus retroflexus L. and Arabidopsis thaliana with an inhibition degree of five. Compound 6d also showed an inhibition degree of five against D. sanguinalis. In addition, at 50 mg/L, most compounds exhibited good in vitro antifungal activity against Sclerotinia sclerotiorum, with compound 6c showing over 90% antifungal activity against S. sclerotiorum and Pellicularia sasakii.     

1,3-二甲基-5-甲硫基-4-苯腙基羰基吡唑的合成及抑菌活性

吡唑衍生物;1;3-二甲基-5-甲硫基-4-苯腙基羰基吡唑的合成及抑菌活性     

Design,synthesis, and bioactivities of novel pyridazinone derivatives containing 2-phenylthiazole or oxazole skeletons

A series of novel pyridazinone derivatives were designed and synthesized by replacing 4-(tert-butyl)phenyl moiety of pyridaben with 2-phenylthiazole or oxazole fragments via activity substructure connecting approach. The structures of all target compounds were characterized through NMR, MS, and elemental analysis. Bioassay results exhibit that most compounds showed potent bioactivities against Aphis fabae, Tetranychus urticae, Erysiphe graminis, and/or Puccinia polysora. Among the newly synthesized compounds, 2-(tert-butyl)-4-chloro-5-(((2-phenylthiazol-4-yl)methyl)thio)pyridazin-3(2H)-one ( 12b ) displays remarkable insecticidal activity against A fabae. Its LC₅₀ value (2.73 mg/L) is better than that of pyridaben (5.46 mg/L), although inferior to that of imidacloprid (0.51 mg/L). In addition to its extraordinary insecticidal activity, compound 12b also exerts 96.9% fungicidal activities against P polysora at 500 mg/L in vivo, significantly superior to that of pyridaben (50.0%), while slightly lower than that of tebuconazole (100%). This article discusses the synthesis, bioassay results, and structure-activity relationship of this series of novel pyridazinone derivatives.     

Cytotoxic and insecticidal activities of derivatives of harmine, a natural insecticidal component isolated from Peganum harmala

In a continuing effort to develop novel β-carbolines endowed with better insecticidal activity, a simple high-yielding method for the synthesis of harmine compounds starting from L-tryptophan has been developed and a series of 1,3-substituted β-carboline derivatives have been synthesized and evaluated for their cytotoxicity against insect cultured Sf9 cell line in vitro and insecticidal activities against 4th instar larvae of mosquitos, Culex pipiens quinquefasciatus and mustard aphid, Lipaphis erysimi. The results demonstrated that 1-phenyl-1,2,3,4-tetrahydro-β-carboline-3-carboxylic acid (compound 2) and methyl 1-phenyl-β-carboline-3-carboxylate (compound 13) represented the best potential compounds, with Sf9 cells inhibition rates of 71.55% and 60.21% after 24 h treatment at concentrations of 50-200 mg/L, respectively. Both compounds 2 and 13 also showed strong insecticidal activity towards 4th instar larvae of mosquitos with LC(50) values of 20.82 mg/L and 23.98 mg/L, and their LC(90) values were 88.29 mg/L and 295.13 mg/L, respectively. Furthermore, the LC(50) values of compounds 2 and 13 against mustard aphids were 53.16 mg/L and 68.05 mg/L, and their LC(90) values were 240.10 mg/L and 418.63 mg/L after 48 h treatment. The in vitro cytotoxicity of these compounds was consistent with the insecticidal activity in vivo. The results indicated that the 1- and 3-positions of the β-carboline ring deserve further investigation to develop biorational insecticides based on the natural compound harmine as a lead compound.     

Synthesis,Crystal Structure and Biological Activities of Novel Anthranilic(Isophthalic) Acid Esters

In search of environmentally benign insecticides with high activity, low toxicity and low resistance, a series of novel anthranilic(isophthalic) acid esters was designed and synthesized based on the structure of ryanodine modulating agent. All the compounds were characterized by ¹H NMR spectra, elemental analysis or high resolution mass spectrometry(HRMS). The preliminary results of biological activity assessment indicate that some of the title compounds exhibit certain but unremarkable insecticidal activity against Mythimna separata Walker at 200 mg/L and fungicidal activities against five funguses at 50 mg/L.