当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Diastereoselective synthesis of potent antimalarial cis-β-lactam agents through a [2 + 2] cycloaddition of chiral imines with a chiral ketene.

Diastereoselective synthesis of potent antimalarial cis-β-lactam agents through a [2 + 2] cycloaddition of chiral imines with a chiral ketene.

Abstract：

:The effect of double asymmetric induction for the synthesis of new cis-β-lactams by [2 + 2] cycloaddition reactions of chiral imines with a chiral ketene was investigated. The cycloaddition reaction was found to be totally diastereoselective leading exclusively to the formation of the cis-β-lactam derivatives. The newly synthesized cycloadducts were evaluated for their antimalarial activities against Plasmodium falciparum K14 resistant strain with moderate to excellent IC50 values varying from 8 to 50 μM. Of the fifteen β-lactams tested, four showed IC50 ≤ 11 μM.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Jarrahpour A,Ebrahimi E,Sinou V,Latour C,Brunel JM

doi

10.1016/j.ejmech.2014.09.077

subject

Has Abstract

pub_date

2014-11-24 00:00:00

pages

364-71

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(14)00896-4

journal_volume

87

pub_type

杂志文章

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