Synthesis And Biological Activity Of Compounds Containing 1,2,4-triazole And 1,3,4-thiadiazole Amides

1,2,4-triazole, 1,3,4-thiadiazole amide derivatives were class of compounds having important applications and good biological activit and had been in the field of pesticides. In this paper, two synthetic routes were designed to afford a series of 1,2,4-triazole and 1,3,4-thiadiazole amide derivatives. And then those target products had been identified by 1H NMR, 13 C NMR, IR, ESI-MS, elemental analysis.The target compounds activities were tested against six important phytopathogenic fungi, namely, Cytospora mandshurica, Phytophthora infestans, Gibberella zeae, Paralepetopsis sasakii, Fusarium oxysporum, Sclerotinia sclerotiorum with growth rate method.The results showed that those target compounds have a certain inhibitory activity against six kinds of fungi. At the concentration of 50 μg/m L, which are lower than standard reagent hymexazol.The target compounds activities were evaluated against three important phytopathogenic bacteria, namely, Xanthomonas axonopodi, Ralstonia solanacearum, Xanthomonas oryzae from by the turbid meter test in vitro. Its bioassay results showed that those target compounds exhibited certain antibacterial activities against three kinds of bacteria. Remarkably, at the concentration of 200 μg/mL, compound Ⅰ3,Ⅰ7,Ⅰ8,Ⅰ10,Ⅰ12 andⅠ23 have good antibacterial activity, inhibition rates were 81.2%, 80.4%, 92.2%, 82.6%, 85.6%, 90.4%; at the concentration of 200 μg/m L, compound Ⅰ3, Ⅰ5, Ⅰ8, Ⅰ12, Ⅰ22 andⅠ23 have some inhibition rate at about 60% against R. solanacearum(at 200 μg/mL, standard reagent thiodiazole-copper inhibition rates was 100%); Meanwhile, at the concentration of 200 μg/m L, there are two compounds(Ⅰ8, Ⅰ10) perform better inhibitions against X. axonopodis, they respectively exhibited inhibition at 97.6%, 93.9%.The half leaf dry spot method was used to test against Tobacco mosaic virus(TMV) activity of the target compounds. The preliminary bioassay results indicated the compounds(Ⅰ3,Ⅰ7,Ⅰ10) containing morpholine showed certain antiviral activity against TMV at a concentration of 500 μg/mL. In terms of effect, compounds Ⅰ3, Ⅰ7 andⅠ10 respectively exhibited inhibition from 26.0% to 42.3%, which are lower than standard reagent Ningnanmycin.