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通过3-巯基-2-丁酮与取代硅基丙炔酸甲酯的环合、酯的选择性水解、异硫氰化、胺化等步骤合成了13个未见报道的噻吩甲酰硫脲衍生物.各噻吩甲酰硫脲衍生物的结构经~1H NMR、~(13)C NMR和元素分析的确证,其对小麦全蚀病、水稻纹枯病病原菌的抑菌活性经平皿法进行了测试.结果表明,大部分噻吩甲酰硫脲衍生物对小麦全蚀病病原菌具有一定抑制活性,其中1-环丙基-3-(4,5-二甲基噻吩-3-甲酰基)硫脲(8c)抑菌活性表现较为突出,在10 mg/L浓度下其抑菌活性接近对照硅噻菌胺的水平.结构分析表明噻吩-3-甲酰硫脲衍生物噻吩环2位官能团的大小对小麦全蚀病菌抑制活性的影响不明显.
Thirteen thiourea thioureas were synthesized by cyclization of 3-mercapto-2-butanone with substituted silylpropiolactone, selective hydrolysis of ester, isothiocyanate, and amination. The structures of each thiophenecarbohydrazide derivatives were confirmed by ~ 1H NMR, ~ (13) C NMR and elemental analysis. Their antibacterial activities against total eclipse of wheat and rice sheath blight were determined by the plate method The results showed that most of the derivatives of thiophenecarbohydrazide had some inhibitory activity against the pathogen of wheat eclipses, in which 1-cyclopropyl-3- (4,5-dimethylthiophene-3-formyl) The antibacterial activity of thiourea (8c) was prominent, and its antibacterial activity at the concentration of 10 mg / L was close to that of the control silithiamine.The structural analysis showed that the thiophene-3-carbonyl thiourea derivative Had no obvious effect on the inhibitory activity of total eclipses in wheat.