Abstract
New thiophene formyl thiourea derivatives were synthesized via cycloaddition reaction of 3-mercaptobutan-2- one and methyl 3-(substitutedsilyl)propiolate, selective hydrolysis of ester, isothiocyanatation and amination. Their chemical structures were confirmed by 1 H NMR, 13 C NMR and elemental analysis. The inhibitory activity against Gaeumannomyces graminis var. tritici and Rhizoctonia solani was evaluated in vitro by the plate method. The results indicated that most of thio- phene formyl thiourea derivatives showed some inhibitory activity against gaeumannomyces graminis var. tritici. Compound 1-cyclopropyl-3-(4,5-dimethylthiophene-3-carbonyl)thiourea (8c) gave the best performance and its inhibitory activity was close to the control level of silthiopham in the concentration of 10 mg/L. The structure analysis showed that the steric hin- drance of functional group at the second position of the thiophene formyl thioureas had no obvious effect on the inhibitory activity against gaeumannomyces graminis var. tritici. Keywords thiophene formyl thiourea derivatives; synthesis; inhibitory activity
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