Synthesis and antimalarial evaluation of cyclic β-amino acid-containing dipeptides

被引：12

作者：

Sathe, Manisha ^{[1
]}

Thavaselvam, Duraipandian ^{[2
]}

Srivastava, Ashish Kumar ^{[1
]}

Kaushik, Mahabir Parshad ^{[1
]}

机构：

[1] Def Res & Dev Estab, Discovery Ctr, Gwalior 474002, India

[2] Def Res & Dev Estab, Div Microbiol, Gwalior 474002, India

来源：

MOLECULES | 2008年 / 13卷 / 02期

关键词：

beta-Lactam; beta-amino acid; antimalarial; Plasmodium falciparum; Plasmodium berghai;

D O I：

10.3390/molecules13020432

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

This paper describes an efficient synthesis and the antiparasitic evaluation of cyclic beta-amino acid-containing dipeptides 3.1-3.6 and 4.1-4.5. The antimalarial properties of all these dipeptides have been evaluated in vitro against Plasmodium falciparum and in vivo against Plasmodium berghai. Compounds 4.4 and 4.5 have been found to be very effective in this respect, with IC50 values of 3.87 and 3.64 mu g/mL in the in vitro test, while 4.5 has also been found to be active in the in vivo evaluation.

引用

页码：432 / 443

页数：12

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