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

Posted on:2017-11-18Degree:MasterType:Thesis
Country:ChinaCandidate:Y ZhouFull Text:PDF
GTID:2351330503471357Subject:Organic Chemistry
Abstract/Summary:PDF Full Text Request
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 ?g/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 ?g/mL, compound ?3,?7,?8,?10,?12 and?23 have good antibacterial activity, inhibition rates were 81.2%, 80.4%, 92.2%, 82.6%, 85.6%, 90.4%; at the concentration of 200 ?g/m L, compound ?3, ?5, ?8, ?12, ?22 and?23 have some inhibition rate at about 60% against R. solanacearum(at 200 ?g/mL, standard reagent thiodiazole-copper inhibition rates was 100%); Meanwhile, at the concentration of 200 ?g/m L, there are two compounds(?8, ?10) 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(?3,?7,?10) containing morpholine showed certain antiviral activity against TMV at a concentration of 500 ?g/mL. In terms of effect, compounds ?3, ?7 and?10 respectively exhibited inhibition from 26.0% to 42.3%, which are lower than standard reagent Ningnanmycin.
Keywords/Search Tags:1,2,4-triazole, Aryloxymethyl, 1,3,4-thiadiazole amide, biologically active
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