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针对烟草花叶病毒(tobacoo mosaic virus,TMV),设计、合成了一系列5-胺基-1-(3-氯-2-吡啶基)-4-(5-甲硫基-1,3,4-噁二唑-2-基)-吡唑衍生物.初步抗TMV活性测试结果表明,大部分化合物对TMV表现出良好的治疗活性,其中化合物T_2、T_(11)和T_(13)在500μg/mL的浓度下,对TMV的治疗活性分别达到58.5%、56.1%和51.2%,略优于对照药剂宁南霉素(51.0%).进一步活性测试表明,化合物T_(11)对TMV的治疗活性的半数有效浓度(EC_(50))值为268.2μg/mL,与宁南霉素(247.2μg/mL)相当.活性化合物T_(11)与TMV外壳蛋白(TMV CP)作用的微量热泳动实验和荧光光谱实验均表明,该化合物与TMV CP之间具有较强的相互作用.
A series of 5-amino-1- (3-chloro-2-pyridyl) -4- (5-methylthio-1,3-benzothiazol- 4-oxadiazol-2-yl) -pyrazole derivatives. The results of preliminary anti-TMV activity tests showed that most of the compounds showed good therapeutic activity against TMV. Compounds T_2, T_ (11) and T_ The therapeutic activity against TMV reached 58.5%, 56.1% and 51.2% at the concentration of 500μg / mL, which was slightly better than that of Ningnanmycin (51.0%). The further activity test showed that the activity of T_ (11) against TMV The median effective concentration (EC50) of the therapeutic activity was 268.2 μg / mL, which was comparable to that of Ningnanmycin (247.2 μg / mL) .Thermal calorific effect of active compound T_ (11) on TMV coat protein (TMV CP) The results of electrophoresis and fluorescence spectroscopy show that there is a strong interaction between this compound and TMV CP.