摘要：In recent years,the damage caused by soil nematodes has become increasingly serious;however,the varieties and structures of the nematicides available on the market are ***,a succinate dehydrogenase inhibitor(SDHI)fungicide developed by Bayer AG in Germany,has been widely used in the prevention and control of soil nematodes due to its high efficiency and novel mechanism of *** this paper,two series of novel target compounds were designed and synthesized with nematicidal and fungicidal fluopyram as the molecular skeleton in order to introduce sulfide and sulfone *** structures were identified and characterized by 1H nuclear magnetic resonance(NMR),13C NMR,and high-resolution mass spectrometer(HRMS).The bioassays revealed that most of the compounds showed excellent nematicidal activities at 200 lg
mL-1 in comparison with fluopyram,while the nematode mortality rate dropped sharply at 100μg·mL-1,except for compounds I-11 and *** terms of fungicidal activity,compound I-9 was discovered to have an excellent inhibitory rate,and a molecular docking simulation was performed that can provide important guidance for the design and exploration of efficient fungicidal lead compounds.

摘要：In an attempt to search for potent fungicide,a series of novel N-ary 1-1H-pyrazole-5-carboxylate derivatives was designed and *** chemical structures were characterized by 1H NMR spectra and high reso・lution mass spectrometry(HRMS).The preliminary bioassay results indicated that some target compounds displayed better fungicidal activities against certain fungi at 50μg/mL or favorable antitumor activities at 5 μg/mL compared with chlorothalonil and 5-fluorouracil,*** structure-activity relationship demonstrated that the introduction of ester group and amide bond was favorable to the improvement of activities against Physalospora pin cola and Phytophthora capsici.

摘要：To discover novel strobilurins analogues with good and broad spectrum activity,a series of nove 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides-based strobilurins was designed,synthesized,and tested agains various phytopathogenic *** *** 7k exhibited substantial and broad spectrum antifungal activities against the tested phytopathogenic fungi,especially compound 7b,which showed 100%,80%,90%,and 90%antifungal activity(in virto)against Erysiphe graminis(***),Puccinia sorghi Schw:(P sorghi Schw.)Colletotrichum lagenarium(***),and Pseudoperonospora cubensis(P cubensis)at 300 ug/mL,*** or comparable to the positive control ***,compound 7b exhibited 85%greenhouse *** activity(in vivo)against *** even at 0.2μg/mL,equal to azoxystrobin(90%)and trifloxystrobin(90%)Meanwhile,compound 7b against P cubensis displayed 70%and 55%greenhouse inhibition activity(in vivo)at 1.56 and 0.2μg/mL,respectively,much better than those of azoxystrobin and trifloxystrobin(both 0%at 1.56 and 0.2 ug/mL).Therefore,compound 7b could be considered as the most promising fungicidal candidate for furthe ***,based on the effective concentration(ECso)against ***,the built CoMSIA model provided the useful reference for the further structural optimization design.

摘要：Eleven 1-(1H-1,2,4-triazole)-2-(2,4-diflurophenyl)-3-(N-methyl-N-substituted benzylamino)-2-propanols were designed and synthesized, on the basis of the crystal structure of P450 cytochrome 14α-sterol demethylase(CYP51) and the docking results of inhibitors to the active site of the enzyme. All title compounds were first by reported. Results of preliminary biological tests showed that most of title compounds exhibited activity against the seven common pathogenic fungi. Compound 11 showed best antifungal activity with broad antifungal spectrum and proved to be more active against Cryptococcus neoformans, Candida albicans, Microsporum lanosum and Trichophyton rubrum than ketoconazole. Compounds 3, 10 and 4 also had high activities.