| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1397623 | European Journal of Medicinal Chemistry | 2011 | 8 Pages |
A facile and one-pot synthesis of a series of novel spiropyrrolidines/pyrrolizidines with β-lactam substituent has been accomplished through 1,3-dipolar cycloaddition reaction of alkenyl esters derived from β-lactam aldehyde as dipolarophile with the dipole azomethine ylide derived from 1,2- and 1,3-diketones and secondary amino acids. The synthesized compounds were evaluated for antimicrobial activities and found to exhibit relatively good antibacterial activity at lower concentration against four human bacterial pathogens.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slideResearch highlights► A series of β-lactam fused spiropyrrolidineds was synthesized by 1,3-dipolar cycloaddition reaction. ► The compounds were found to have antibacterial activity against selected pathogens. ► Some of the compounds were found to have better activity than the reference compound tetracycline. ► The grafting of β-lactam with pyrrolidine unit has enhanced the overall bioactivity of the products.
