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Synthesis, Structure and H+/K+-ATPase Inhibitory Activity of Novel Triazolyl Substituted Tetrahydrobenzofuran Derivatives via One-pot Three-component Click Reaction
- Source :
- Chinese Journal of Chemistry. 31:831-836
- Publication Year :
- 2013
- Publisher :
- Wiley, 2013.
-
Abstract
- Eleven triazolyl substituted tetrahydrobenzofuran derivatives were synthesized in high yields as novel H+/K+-ATPase inhibitor via one-pot CuI-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, elemental 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 µmol·L−1. The initial structure-activity analysis suggested that the triazole substituted by cycloalkyl, aromatic ring or O-containing side-chain seemed to be beneficial for enhancing the activity.
Details
- ISSN :
- 1001604X
- Volume :
- 31
- Database :
- OpenAIRE
- Journal :
- Chinese Journal of Chemistry
- Accession number :
- edsair.doi...........d29391675128c7e7294b41486accbb91