Eleven triazolyl substituted tetrahydrobenzofuran derivatives were synthesized in high yields as novel H＋/K＋- ATPase inhibitor via one-pot Cul-catalyzed three-component click reaction of azide, secondary amine and 3...Eleven triazolyl substituted tetrahydrobenzofuran derivatives were synthesized in high yields as novel H＋/K＋- ATPase inhibitor via one-pot Cul-catalyzed three-component click reaction of azide, secondary amine and 3-bromopropyne under mild conditions in water. Their structures were characterized by NMR, IR, ESI-MS, ele- mental analysis and single-crystal X-ray diffraction analysis. Most of the target compounds exhibited better H＋/K＋- ATPase inhibitory activity than commercial omeprazole with IC50 values less than 15 gmol＇L-~. The initial struc- ture-activity analysis suggested that the triazole substituted by cycloalkyl, aromatic ring or O-containing side-chain seemed to be beneficial for enhancing the activity.展开更多
文摘Eleven triazolyl substituted tetrahydrobenzofuran derivatives were synthesized in high yields as novel H＋/K＋- ATPase inhibitor via one-pot Cul-catalyzed three-component click reaction of azide, secondary amine and 3-bromopropyne under mild conditions in water. Their structures were characterized by NMR, IR, ESI-MS, ele- mental analysis and single-crystal X-ray diffraction analysis. Most of the target compounds exhibited better H＋/K＋- ATPase inhibitory activity than commercial omeprazole with IC50 values less than 15 gmol＇L-~. The initial struc- ture-activity analysis suggested that the triazole substituted by cycloalkyl, aromatic ring or O-containing side-chain seemed to be beneficial for enhancing the activity.
