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1.
Yitao Li Wenqiang Yao Jian Lin Falin Li Yang Wu Junxing Xu 《Journal of heterocyclic chemistry》2019,56(8):2170-2178
The triazole sulfonamide played a very important role in the field of research of new agrochemical compounds as a novel heterocyclic compound with lack of reported resistance. For the research on the innovative triazole sulfonamide fungicide effective against cucumber downy mildew (CDM), the present article designed an array of 1,2,4‐triazole‐1,3‐disulfonamide derivatives. The derivatives were synthesized via coupling multiple benzylamine with triazole sulfonamide groups. 1H‐NMR, 13C‐NMR, and LC–MS spectrometry were used to characterize these synthesized compounds. Most of these derivatives exhibited better fungicidal activities than that of the commercial cyanosole using bioassays. In particular, compounds 6g and 6h showed the best fungicidal activity against CDM (EC50 = 6.91 and 10.62 mg/L). Comparative experiments demonstrated that the fungicidal activity of 6g and 6h was better than the commercial pesticides amisulbrom and cyanosole. According to the study, the compound 6g had a giant application potential on fungicide against CDM. 相似文献
2.
A series of novel pyrazole oxime derivatives containing oxazole ring were designed and synthesized. The title compounds were structurally confirmed by 1H NMR, 13C NMR spectra and elemental analyses. Preliminary bioassay results showed that some of the title compounds displayed promising fungicidal activity besides insecticidal and acaricidal activity. Particularly, compound 8c exhibited potent fungicidal activity against cucumber Pseudoperonospora cubensis beyond good insecticidal activity against Aphis craccivora and Nilaparvata lugens. 相似文献
3.
AbstractPhenazine-1-carboxylic acid (PCA) as a natural product which has significant inhibition effects against many soil-borne fungal phytopathogens in agricultural application and has been registered in China as the fungicide against rice sheath blight. In order to find new higher fungicidal activities lead compounds and develop new eco-friendly agrochemicals, we introduced substructure piperazines which also have high biological activity into PCA, designed and synthesized a series of phenazine-1-carboxylic piperazine derivatives, and their structures were confirmed by 1H NMR and HRMS. Most compounds exhibited certain in vitro fungicidal activities. In particular, Compounds 5r exhibited the activity against all the tested pathogenic fungi, such as Rhizoctonia solani, Alternaria solani, Fusarium oxysporum, Fusarium graminearum, Pyricularia oryzac Cavgra, with the EC50 value of 24.6μM, 42.9μM, 73.7μM, 73.8μM, 34.2μM, respectively, more potent activities than PCA (33.2μM, 81.5μM, 186.5μM, 176.4μM, 37.3μM). This result provided a highly active lead compound for the further structure optimization design. 相似文献
4.
Nine novel 2-methyl-4-trifluoromethylthiazole-5-carboxamide derivatives were designed and synthesized utilizing ethyl 4,4,4-trifluoroacetoacetate as a starting material. Subsequently, the biological activity of the compounds was evaluated in the greenhouse. Results indicated that all of the compounds have some fungicidal and insecticidal activity but no herbicidal activity. Compound 1 has fungicidal activity with 90% control of tomato late blight at 375 g ai/ha, while two compounds 2F and 2H show insecticidal activity with 80 and 100% control, respectively, against potato leafhopper at 600 g ai/ha. 相似文献
5.
Yitao Li Jian Lin Wenqiang Yao Guoliang Gao Dewang Jing Yang Wu 《Journal of heterocyclic chemistry》2020,57(5):2128-2138
Downy mildew is a very important detrimental disease that lead reduced to fruits and vegetables. Due to the continuous growth of drug resistance, finding novel fungicides with dissimilar modes of function from present fungicides for controlling downy mildew are imminent. This work is an extension of our preceding research on the original triazole sulfonamide derivatives lead compound. Triazole sulfonamide as a remarkable nitrogen-containing heterocyclic compound opposed cucumber downy mildew (CDM) develops a quite vital part in the sphere of the study of new farm chemicals. The existing report designs a certain amount of 1,2,4-triazole-1,3-disulfonamide derivatives. Hydrazones have obtained extensive attention in the field of pharmaceutical due to its unique chemical structure and remarkable activity (insecticidal, antibacterial, antifungal and herbicidal). By means of coupling numerous hydrazone with triazole sulfonyl chloride groups, 24 novel derivatives were synthesized. Spectrum analysis of LC-MS, 1H NMR and 13C NMR were used for characterizing these new compounds. Compared with commercial Cyazofamid using bioassays, most of these compounds displayed preferable fungicidal activities. Moreover, compounds 8q illustrated the greatest CDM resistance (EC50 = 7.776 mg/L). Field efficacy trials revealed that compound 8q fungicidal activity was higher than the purchased agrochemical Cyazofamid and Amisulbrom. Thus, the research declared that 8q displayed a great potential for the application of fungicide against CDM. 相似文献
6.
Liu Meng De-Qing Shi 《Phosphorus, sulfur, and silicon and the related elements》2013,188(9):2314-2323
A series of title compounds 2 were efficiently synthesized via the condensation of 1-phenyl-2-(1H-1,2,4-triazol-1-yl)ethanone oxime with various asymmetric thiophosphoryl chlorides in sodium hydroxide powder and acetonitrile system. The structures of title compounds 2 were confirmed by IR, 1H NMR, 31P NMR, EI-MS, and elemental analysis. The results of preliminary bioassays indicated that the title compounds 2 possessed good to moderate insecticidal activity against aphides at the dosage of 250 mg/L, and some of them exhibited moderate fungicidal activities at the concentration of 100 mg/L. 相似文献
7.
Iván Montenegro 《Natural product research》2019,33(8):1214-1217
A series of novel dihydrochalcone derivatives 2–7 were synthesized from dihydroisorcordoin 1 which was isolated from the aerial parts of Adesmia balsamica. The structures of all compounds were confirmed by 1H NMR, 13C NMR, and HRMS. Their anti-oomycete activity was evaluated in vitro against Saprolegnia parasitica and Saprolegnia diclina. Some of the newly synthesized compounds exhibited better anti-oomycete activities at low values compared with bronopol and fluconazole as positive controls. Among them, compound 7 exhibited strong activity, with minimum inhibitory concentration and minimum oomyceticidal concentration values of 75 and 100 μg/mL, respectively. 相似文献
8.
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
9.
Qiao-Xia Liu Ming-Zhen Mao Li-Xia Xiong Zheng-Ming Li 《Phosphorus, sulfur, and silicon and the related elements》2013,188(9):593-599
AbstractA series of novel anthranilic diamide derivatives containing pyridylpyrazole and iminodithiocarbamate or thiosemicarbazone motifs were synthesized via multi-step reactions. The structures of seven title compounds (methyl 2-(2-(3-bromo-1-(3-chloropyridin-2-yl)-1H-pyrazole-5-carboxamido)-5-chloro-3- methylbenzylidene)hydrazinecarbodithioate 7 and 3-bromo-N-(2-((2-substitutedcarbamothioylhydrazono)methyl)-4-chloro-6-methylphenyl)-1-(3-chloropyridin-2-yl)-1H-pyrazole-5-carboxamide 8a-8f) were confirmed by melting points, IR, 1H NMR, 13C NMR, and HRMS. The bioassays showed that some of the compounds exhibited modest insecticidal activities against oriental armyworm (Mythimna separata Walker), particularly, compound 8b (3-bromo-N-(4-chloro-2-methyl-6-((2-(methylcarbamothioyl)hydrazono)methyl)phenyl)-1-(3-chloropyridin-2-yl)-1H-pyrazole-5-carboxamide) held 100% and 30% larvicidal activity at the concentration of 25?mg/L and 10?mg/L, respectively. In addition, several compounds displayed favorable fungicidal activities against Alternaria solani Sorauer and Physalospora piricola at 50?μg/mL, and were comparable with the controls Chlorothalonil and Triadimefon. The results in this paper will provide important information for further research and development of sulfur-containing heterocyclic agrochemicals. 相似文献
10.
Shan Yang Tienan Wang Yanan Zhou Li Shi Aidang Lu Ziwen Wang 《Molecules (Basel, Switzerland)》2021,26(2)
Based on the structure of the natural product cysteine, a series of thiazolidine-4-carboxylic acids were designed and synthesized. All target compounds bearing thiazolidine-4-carboxylic acid were characterized by 1H-NMR, 13C-NMR, and HRMS techniques. The antiviral and antifungal activities of cysteine and its derivatives were evaluated in vitro and in vivo. The results of anti-TMV activity revealed that all compounds exhibited moderate to excellent activities against tobacco mosaic virus (TMV) at the concentration of 500 μg/mL. The compounds cysteine (1), 3–4, 7, 10, 13, 20, 23, and 24 displayed higher anti-TMV activities than the commercial plant virucide ribavirin (inhibitory rate: 40, 40, and 38% at 500 μg/mL for inactivation, curative, and protection activity in vivo, respectively), especially compound 3 (inhibitory rate: 51%, 47%, and 49% at 500 μg/mL for inactivation, curative, and protection activity in vivo, respectively) with excellent antiviral activity emerged as a new antiviral candidate. Antiviral mechanism research by TEM exhibited that compound 3 could inhibit virus assembly by aggregated the 20S protein disk. Molecular docking results revealed that compound 3 with higher antiviral activities than that of compound 24 did show stronger interaction with TMV CP. Further fungicidal activity tests against 14 kinds of phytopathogenic fungi revealed that these cysteine derivatives displayed broad-spectrum fungicidal activities. Compound 16 exhibited higher antifungal activities against Cercospora arachidicola Hori and Alternaria solani than commercial fungicides carbendazim and chlorothalonil, which emerged as a new candidate for fungicidal research. 相似文献
11.
Synthesis and Biological Activities of Novel 6‐Alkylamino‐11,12‐dihydro‐11‐arylbenzo[c]phenanthridine Derivatives
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Min Zhang Li Liu Huifeng Xiao Ting Zhao Liuqing Yang Xiaohua Xu 《Journal of heterocyclic chemistry》2016,53(1):234-240
A series of novel benzo[c]phenanthridine derivatives 2a , 2b , 2c , 2d , 2e , 2f , 2g , 2h , 2i , 2j , 2k , 2l , 2m and 3a , 3b , 3c , 3d , 3e , 3f bearing an alkylamino side chain at their 6‐position were synthesized. All of the target compounds were confirmed by 1H NMR, 13C NMR, and HRMS, and some of them were also characterized by IR and 19F NMR. The preliminary bioassays showed that the target compounds displayed fungicidal activities; for example, compound 2l showed 60.0% and 70.0% inhibitive activity against Alternaria solani and Cercospora arachidicola at 50 mg/L, respectively, and some compounds also displayed plant growth‐regulating activities. 相似文献
12.
含1,2,4-三唑杂环的新型Strobilurins衍生物的合成及杀菌活性 总被引:4,自引:0,他引:4
为了寻找新的高活性先导化合物, 设计合成了14个未见文献报道的Strobilurins类衍生物, 结构经MS, 1H NMR, 元素分析确认. 并用X-ray单晶衍射测定了(E)-3-甲氧基-2-[(5-甲基-4-邻溴代苯亚甲基亚胺基-1,2,4-三唑)-3-硫亚甲基]-苯基丙烯酸甲酯(5i)的晶体结构, 证实了分子中的两个C=C均为E-式构型. 初步生物活性测试结果表明, 在实验浓度下部分化合物具有一定的杀菌活性. 相似文献
13.
WAN Jun LI Chun-li LI Xue-mei ZHANG Shu-sheng 《高等学校化学研究》2006,22(4):465-467
The title compound was synthesized and characterized by IR, ^1H NMR, elemental analysis and single crystal X-ray diffraction analysis. Its biological activities were also tested. The results show that the title compound reveals inhibiting activities towards wheat gibberellin, apple ringspot, tomato early blight, peanut cercospora arachidicola and stem wilt of asparagus. 相似文献
14.
WAN Jun LI Chun-li LI Xue-mei ZHANG Shu-sheng~ College of Chemistry Molecular Engineering Qingdao University of Science Technology Qingdao P.R. China 《高等学校化学研究》2006,22(4)
IntroductionTriazole derivatives have become the most rapidlyexpanding group of antifungal compounds with advanta-ges of lowtoxicity, high oral bioavailability and broad-spectrum antifungal activity, which can be used againstfungi including most yeasts an… 相似文献
15.
Yongqiang Li Ziwen Wang Pengxiang Zhang Yuxiu Liu Lixia Xiong Qingmin Wang 《Journal of heterocyclic chemistry》2014,51(5):1410-1414
To investigate the alkyl analog of insecticide chlorfenapyr, two series of 2‐alkyl‐4‐bromo‐5‐(trifluoromethyl)pyrrole‐3‐carbonitriles were synthesized with a cycloaddition as the key step. The target products were characterized by 1H‐NMR spectroscopy, elemental analysis, or HRMS. The insecticidal, herbicidal, and antifungal activities of the target compounds were evaluated and found that these compounds did not show much insecticidal activity, but compounds 4 , 10 , and 11 had very good fungicidal activities against Alternaria solani and Fusarium oxysporum. Moreover, compound 4 had an outstanding inhibition effect against pigweed. 相似文献
16.
Design,Synthesis and Biological Activities of Novel Benzoyl Hydrazines Containing Pyrazole 总被引:1,自引:0,他引:1
Tao Yan Shujing Yu Pengfei Liu Zhuo Liu Baolei Wang Lixia Xiong Zhengming Li 《中国化学》2012,30(4):919-923
In search of environmentally benign compounds with high biological activity, low toxicity and low resistance, 8 novel benzoyl hydrazines containing pyrazole were designed and synthesized. All compounds were characterized by 1H NMR spectra and HRMS. The preliminary results of biological activity assessment indicated that most of title compounds exhibited certain insecticidal activities against Mythimna separata Walker at 200 mg·L?1 but excellent fungicidal activities against six fungus at 50 mg·L?1, which were better than the control. 相似文献
17.
18.
N-甲氧基-N-[2-(1,6-2H-1-取代-6-羰基-哒嗪-3-氧甲基)苯基]氨基甲酸甲酯的合成及生物活性研究 总被引:4,自引:3,他引:4
为了寻找高效、低毒的农药, 设计合成了一系列新的N-甲氧基-N-[2-(1,6-2H-1-取代-6-羰基-哒嗪-3-氧甲基)苯基]氨基甲酸甲酯化合物3a~3k, 其结构经IR, 1H NMR, LC/MS和元素分析确认. 生物活性测定表明, 部分化合物在50 mg/L下对小麦赤霉病菌(Gibberella zeae)、稻瘟病菌(Pyricularia oryzae)和黄瓜灰霉病菌(Botrytis cinerea)有较好的抑菌活性. 相似文献
19.
Synthesis and fungicidal activity of novel 1,2,4-triazole derivatives containing a pyrimidine moiety
Wen-Neng Wu Yang-Ming Jiang Qiang- Fei Hai-Tang Du 《Phosphorus, sulfur, and silicon and the related elements》2013,188(12):1171-1175
AbstractA series of novel 1,2,4-triazole derivatives containing a pyrimidine moiety were synthesized and their fungicidal activities were evaluated. The preliminary biological test indicated that some of the target compounds exhibited moderate to good fungicidal activities against the tested plant pathogenic fungi compared with the commercial agent. Among them, compounds 9n and 9o exhibited excellent antifungal activity against Phompsis sp., with the half-maximal effective concentration (EC50) values of 25.4 and 31.6?μg/mL, which were even better than the commercial agent of Pyrimethanil (32.1?μg/mL). Meanwhile, compound 9o showed better fungicidal activities against B. dothidea and B. cinerea with 40.1 and 55.1?μg/mL, respectively, in comparison with that of commercial Pyrimethanil (57.6 and 62.8?μg/mL). 相似文献
20.
Synthesis and Biological Activity of Some Novel Aryl‐Substituted 1,3,4‐Oxadiazole Mannich Bases Containing Pyrimidine Rings
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Shengqiang Shen Xiaohong Sun Yuanfa Liu Bang Chen Ruyi Jin Haixia Ma 《Journal of heterocyclic chemistry》2015,52(5):1296-1301
A series of novel Mannich base derivatives (E1–E15) of 5‐aryl‐1,3,4‐oxadiazole‐2‐thione with substituted pyrimidine were synthesized and characterized by elemental analysis, IR, 1H‐NMR. The antifungal activities of these compounds were also originally studied. The results showed that most of the title compounds exhibited relatively good fungicidal activities. Especially compounds E8 and E13 showed better antifungal activity than comparison compound hymexazol. The relationship of structure and activity revealed that the presence of the methyl group at four and six positions of pyrimidine ring remarkably enhanced the antifungal activity of title compounds. 相似文献