共查询到19条相似文献,搜索用时 78 毫秒
1.
N-(2-(取代苯并噻唑-2-氨基甲酰基)-取代苯基)-4-氟苯甲酰胺衍生物的合成及生物活性 总被引:2,自引:0,他引:2
以对氟苯甲酸和取代邻氨基苯甲酸为起始原料,设计并合成11个含氟基苯并噻唑基邻甲酰氨基苯甲酰胺类化合物,其结构经1 H NMR、13C NMR、IR及元素分析确证.初步生物活性测试结果表明,在500 mg/L浓度下部分化合物对烟草花叶病毒(TMV)有一定抑制作用.采用MTT法进行化合物抑制PC3及Bcap-37癌细胞体外活性测试,结果表明所合成的化合物具有不同程度的抑制PC3和Bcap-37癌细胞活性,其中化合物4d在10 μmol·L-1浓度下对PC3和及Bcap-37的抑制率分别为73.2%和68.1%. 相似文献
2.
3.
2,4-二氟苯甲酸或2-氟苯甲酸与二氯亚砜经酰氯化反应,再与邻氨基苯甲酸反应后在醋酸酐中闭环,最后与取代苯并噻唑胺反应合成了9个新型的N-[2-(取代苯并噻唑-2-氨基甲酰基)苯基]取代氟基苯甲酰胺(6a~6i),其结构经1H NMR,13C NMR,IR和元素分析表征。采用MTT法对6a~6i进行抑制PC3癌细胞体外活性测试,结果表明6a~6i具有不同程度的抑制PC3癌细胞活性,其中10μmol.L-16b对PC3的抑制率为69.9%。 相似文献
4.
5.
为了寻找高活性农药先导化合物,以甲霜灵为先导,通过活性基团拼接原理,设计合成了一系列未见文献报道的双酰胺类化合物,其结构经1H NMR、13C NMR和HRMS表征.初步的生物活性测试结果表明:在50 mg/L测试浓度下,化合物5j对黄瓜霜霉病显示出85%的抑制率;在500 mg/L剂量下,多数目标化合物对粘虫表现出较好的杀虫活性,其中化合物5b,5f,5g,5h,5i,5l对粘虫的致死率高达100%,在250 mg/L测试浓度下,化合物5f,5h,51对粘虫的致死率为50%. 相似文献
6.
7.
8.
9.
10.
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. 相似文献
11.
A series of novel anthranilic diamides containing N-substituted arylmethyl moieties was designed and synthesized, in which the bond distance and conjugation pattern between pyrazole and pyridine rings contained in Chlorantraniliprole were changed. Their structures were confirmed by JH NMR, IR, elemental analysis or high resolution mass spectromentry{HRMS), and the conformation of compound 4d was confirmed by X-ray diffraction. The preliminary bioassay results indicate that all the target compounds exhibited moderate insecticidal activity against oriental armyworm at 200 mg/L and some of them presented favorable antitumor activities against human lung cancer cells(A549), liver cancer cells(BelT402) and colon cancer celIs(HCT-8) in vitro by microculture tetrazolium(MTT) method, among which compound 6j afforded the best anti-proliferative activity at 5μg/mL. 相似文献
12.
LI Huangong ZHAO Yangyang SUN Pengwei GAO Li XIONG Lixia YANG Na ZHOU Sha LI Yuxin LI Zhengming 《高等学校化学研究》2021,37(3):655-661
Aseries of novel anthranilic diamides analogues(9a-9t) containing trifluoroethoxyl pyrazole moiety was designed and synthesized and their insecticidal bioactivities against Mythimna separata(Walker, M. separata) and Plutellaxylostella (P. xylostella) were evaluated. The structures of the title compounds were confirmed by 1H NMR, 13C NMR and HRMS. Preliminary insecticidal activities showed that some of the title compounds possessed good to excellent bioactivities towards M. separata and P. xylostella. Compounds 9c and 9t exhibited 100% mortality rate against M. separate at 0.2 mg/L. For the P. xylostella, the synthesized compounds(9c-9e, 9i and 9o) showed 70%, 80%, 75%, 65% and 60% insecticidal activities at 1×10-6 mg/L, respectively, higher than that of chlorantraniliprole(0). Based on excellent insecticidal activities, the mode of the action was tested by the calcium-imaging technique, the results of which demonstrated that the novel compounds shared the same target with chlorantraniliprole. The binding pose of the most active compound 9t in RyRs of P. xylostella was predicted by molecular docking, which showed that compound 9t interacted with the residues Glu140(A) and His147(A) via hydrogen bond. 相似文献
13.
含1,2,3-噻二唑的邻甲酰胺基苯甲酰胺类化合物的合成、晶体结构与生物活性 总被引:7,自引:0,他引:7
以取代邻氨基苯甲酸为起始原料, 设计并合成了一系列未见文献报道的含1,2,3-噻二唑的邻甲酰胺基苯甲酰胺类化合物. 所有化合物的结构均经元素分析和1H NMR确证, 并且采用X射线单晶衍射分析方法测定了化合物7g的结构. 初步的生物活性试验结果表明, 部分化合物具有一定的杀菌活性. 相似文献
14.
LIU Jingbo LI Yuxin CHEN Youwei WU Changchun WAN Yingying WEI Wei XIONG Lixia ZHANG Xiao YU Shujing LI Zhengming 《高等学校化学研究》2016,32(1):41-48
Anthranilic diamides are one of the most important classes of modern agrochemical insecticides. To discover new structures with higher activity, lower toxicity and lower residue, a series of novel anthranilic diamides containing dihydroisoxazoline and isoxazole was designed and synthesized. Their structures were characterized by means of melting points, proton nuclear magnetic resonance(1H NMR), 13C NMR and high resolution mass spec-trometry(HRMS). According to the bioassay data, it was found that some of the title compounds exhibit moderate insecticidal activity and good antifungal activity. In particularly, compound 15b with a concentration of 50 mg/L shows a lethality rate of 60.0% against Mythimna separata Walker and a lethality rate of 50.0% against Culex pipiens pallens with a concentration of 1mg/L. Moreover, compound 15b showed good antifungal activities(58.8%, 77.1%, 70.7%, 55.3%, 60.7%, 65.4%) when against all the tested fungi(Cercospora arachidicola Hori, Physalospora piricola, Rhizoctonia cerealis, Bipolaris maydis, Watermelon anthracnose, Fusarium moniliforme). The effects of compounds 14h, 14j and 15b on the concentration of intracellular calcium ion([Ca2+]i) in the central neurons of Mythimna separate Walker were well investigated via calcium imaging technique. The results demonstrate that the novel compounds can elevate the calcium concentration in the neurons, denoting that some new structures are potential modulators of the insect ryanodine receptor(RyR). 相似文献
15.
16.
ZHANG Ji-feng LIU Chen LIU Peng-fei YAN Tao WANG Bao-lei XIONG Li-xia LI Zheng-ming 《高等学校化学研究》2013,29(4):714-720
A series of novel anthranilic diamides analogues containing benzo[b]thiophenyl ring was designed and synthesized. Their structures were characterized by melting points, 1H nuclear magnetic resonance(1H NMR) and high-resolution mass spectrometry(HRMS). The bioassay tests indicate that their insecticidal activities were weak to moderate. Antibacterial tests indicate that some of the compounds showed favourable activity in vitro against Physalospora piricola, Alternaria solani, Cercospora arachidicola, Gibberella sanbinetti and Phytophthora infestans at a dosage of 50 mg/L. 相似文献
17.
In order to systematically study the structure-activity relationship of anthranilic diamides and develop insecticides with simple structure and high efficiency, a series of novel anthranilic diamides containing N-H/CH3-1H-pyrazole was designed and synthesized. Their chemical structures were characterized by 1H NMR spectra, high resolution mass spectrometry(HRMS) or 13C NMR spectra. The preliminary bioassay results indicated that all title compounds displayed moderate insecticidal activity against oriental armyworm(Mythimna separata) at 200 mg/L and fungicidal activities against six kinds of fungi at 50 mg/L, especially compound 5i showed 50% insecticidal activity at 25 mg/L. In addition, some compounds exhibited certain antitumor activities. It was demonstrated that the introduction of CH3 group into pyrazole ring was superior to H for the insecticidal activity. 相似文献
18.
Two series of novel anthranilic diamides containing oxime ester and diacylhydrazine moieties were designed and synthesized.Their structures were characterized by melting points,1H NMR,13C NMR and high resolution mass spectrometry(HRMS).The single crystal structure of compound 7e was determined by X-ray diffraction and their evaluated insecticidal activity against oriental armyworm(Mythimna separata) indicates that some of the compounds exhibited moderate insecticidal activities.Among the 20 compounds,6a and 6b show 100% larvicidal activity against Mythimna separate Walker at the test concentration of 100 mg/L. 相似文献
19.
Xuewen Hua Wutao Mao Zhijin Fan Xiaotian Ji Fengyun Li Guangning Zong Haibin Song Kalinina Tatiana Yury Yu. Morzherin Nataliya P. Belskaya Vasiliy A. Bakulev 《Journal of heterocyclic chemistry》2016,53(3):865-875
Three series of new anthranilic diamide derivatives containing sulfide, N‐cyanomethylsulfilimine, and N‐cyanomethylsulfoximine groups were designed and synthesized by combining the active substructures of anthranilic diamides and sulfoxaflor. The structures of all newly synthesized compounds were confirmed by IR and 1H/13C‐NMR, and some of them were confirmed by elemental analysis or HRMS too. The synthesized compounds were screened for their insecticidal and fungicidal activities. Bioasssay results indicated that some of the synthesized compounds possessed certain degrees of insecticidal activity against Mythimna separata. However, some compounds exhibited good fungicidal activity against Sclerotinia sclerotiorum. 相似文献