Synthesis of plasmepsin II inhibitors - Potential antimalarial agents

被引：10

作者：

Mueller, R

Huerzeler, M

Boss, C

机构：

[1] Actel Pharmaceut Ltd, CH-4123 Allschwil, Switzerland

[2] Univ Appl Sci Basel, CH-4132 Muttenz, Switzerland

来源：

MOLECULES | 2003年 / 8卷 / 07期

关键词：

malaria; plasmepsin II; reductive amination; Suzuki coupling;

D O I：

10.3390/80700556

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：

A new series of plasmepsin II (PM II) inhibitors has been prepared based on 4-aminopiperidine-tert-butyl-carbamate (1). These compounds might be useful as antimalarial drugs acting via a new mechanism, and therefore be less susceptible to parasite resistance now often observed with current antimalarial therapies. Some of the final compounds prepared exhibited encouraging inhibitory activity towards PM II.

引用

页码：556 / 564

页数：9

共 14 条

[1] Reductive amination of aldehydes and ketones with sodium triacetoxyborohydride. Studies on direct and indirect reductive amination procedures [J].