Sử dụng vi sóng để tổng hợp, đánh giá hoạt tính và nghiên cứu docking một số dẫn chất 1,3,4-oxadiazol và 1,3,4-thiadiazol

A series of 2-amino-substituted 1,3,4-oxadiazole and 1,3,4-thiadiazole derivatives have been synthesized from semicarbazide or thiosemicarbazide and aldehydes under microwave irradiation. The structures were confirmed by 1H-NMR, 13C-NMR and MS spectra. All the synthesized compounds were screened for in vitro antibacterial and antifungal activities by the disk-diffusion method. The anticancer activities were evaluated by MTT assay. Compound (1b) showed high antibacterial activity against MSSA and MRSA (4-16 µg/mL). Compound (2d) showed high antifungal activity against Aspergillus niger (128 µg/mL). Compounds (2c-d) exhibited medium cytotoxic activity and is non-toxic on normal cell lines, which is comparable to the activity of paclitaxel.
Keywords: 1,3,4-oxadiazole, 1,3,4-thiadiazole, antibacterial, antifungal and anticancer activities.