关键词: 2,5-二取代-1,3,4-噻二唑, 生物活性, 一锅法合成, 相转移催化, 超声波辐射

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.

Key words: one-pot synthesis, biological activity, ultrasonic irradiation, phase transfer catalysis, 2,5-disubstituted-1,3,4-thiadiazole