The triazolo-methyl tetrahydrobenzofuran oxime ether isomers were prepared through Cu (II)-catalyzed Huisgen 1,3-dipolar cycloaddition reaction in a high-yielding three-step reaction sequence under mild conditions. All of the intermediates and target compounds were characterized by NMR, IR, ESI-MS and elemental analysis. Thein vitroanti-ulcer activity evaluation indicated the (Z)-oxime isomer of triazolo-methyl tetrahydrobenzofuran oxime ether exhibited most potent H+/K+-ATPase inhibitory effect with the IC50˰̵̱̼͆ͅ˰̶̿˰̅˾́̅˰μ ̝˾ These compounds could be potentially used as anti-ulcer agents for the treatment of acid related diseases.
Five novel bisabolonalone hydrazone carboxamides were synthesized as potential anti-ulcer agents. Their structures were characterized by NMR, IR and ESI-MS. All of the compounds possessed the better H+/K+-ATPase inhibitory activity than the commercial omeprazole with the IC50 of 18~68 μM in vitro. These compounds could be potentially use for the treatment of ulcer related diseases.
A series of four 3-acyl-5-hydroxybenzofuran derivatives (4a-4d) were synthesized by one-pot method under microwave irradiation from aldehydes, dimethylformamide dimethyl acetal (DMFA) and benzoquinone in high yields. These compounds were characterized by IR, NMR and ESI-MS, which were also tested for in vitro anti-proliferative activity against human breast cancer ER(+)-MCF-7 and ER(-)-MDA-MB-231 cell lines. The bioactive compound 4d exhibited the best anti-breast cancer activity against MCF-7 cells with the IC50 values of 43.08 μM. The compound might be used as a potential anti-tumor agent for the further structure modifications and development.
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