2,5-二取代－1,3,4-噻二唑衍生物的一锅法合成、结构表征及生物活性研究

A facile one-pot synthesis of 2,5-disubstituted-1,3,4-thiadiazoles was achieved by ultrasonic irradiation and phase transfer catalysis for the first time and eight novel 2,5-disubstituted-1,3,4-thiadiazoles were synthesized. This method has the advantages of mild conditions, short time, good yields, convenience, economy and environmental friendliness. The structures of the target molecules were characterized by IR, 1H NMR, 13C NMR, 1D NOE, MS spectra and elemental analysis. The experiments of the biological activity for the target molecules were accomplished. The experimental results of the inhibiting activity against COX-2 indicated that the compound 5f had the highest inhibition rate, up to 95.59%, and yet the compound 5g exhibited weakly inhibiting activity. The target compounds did not possess anticonvulasional activity.