Diastereoselective Synthesis of Potent Antimalarial <i>Cis</i>-β-lactam Agents
| Author | Aliasghar Jarrahpour | en |
| Author | Maryam Rostami | en |
| Author | Véronique Sinou | en |
| Author | Christine Latour | en |
| Author | Lamia Djouhri-Bouktab | en |
| Author | Jean Michel Brunel | en |
| Issued Date | 2019-04-30 | en |
| Abstract | Fifteen novel β-lactams bearing N-ethyl tert-butyl carbamate group 5a-o and fifteen N-(2- aminoethyl) β-lactams 6a-o were synthesized by [2+2] ketene-imine cycloaddition reaction (Staudinger). The cycloaddition reaction was found to be totally diastereoselective leading exclusively to theformation of cis-β-lactam derivatives. These newly synthesized β-lactams were evaluated for their antimalarial activity against p. falciparum K14 resistant strain and showed good to excellent EC50 values. Of the thirty β-lactams tested, 5 h, 6a and 6c showed IC50 < 20 µM while 5b, 5c, 5e, 5f, 5g, 5i, 5j, 6d, 6g and 6h exhibited IC50 | en |
| DOI | https://doi.org/10.22037/ijpr.2017.2024 | en |
| Keyword | N-(2-aminoethyl) β-lactams | en |
| Keyword | tert-butyl carbamate | en |
| Keyword | 2-Azetidinones | en |
| Keyword | <i>P. falciparum</i> | en |
| Keyword | Staudinger | en |
| Keyword | Antimalarial activity | en |
| Publisher | Brieflands | en |
| Title | Diastereoselective Synthesis of Potent Antimalarial <i>Cis</i>-β-lactam Agents | en |
| Type | Original Article | en |
Files
Original bundle
1 - 1 of 1
Loading...
- Name:
- ijpr-18-596.pdf
- Size:
- 538.55 KB
- Format:
- Adobe Portable Document Format
- Description:
- Article/s PDF