Quinoline antimalarials

被引：55

作者：

Egan, TJ ^{[1
]}

机构：

[1] Univ Cape Town, Dept Chem, ZA-7701 Rondebosch, South Africa

来源：

EXPERT OPINION ON THERAPEUTIC PATENTS | 2001年 / 11卷 / 02期

关键词：

aminoquinoline; antimalarial; chloroquine; malaria; mechanism; quinoline; resistance;

D O I：

10.1517/13543776.11.2.185

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Quinoline antimalarial patents and relevant scientific literature concerning their mechanism of action, mechanism of resistance and structure-function relationships are discussed in this review. The review provides a brief history of current antimalarial drugs and describes some salient features about their use, occurrence of drug resistance, their metabolism and known adverse effects. Recent advances in our understanding of the mechanism of action of 4-aminoquinolines, quinoline methanols and 8-aminoquinolines are discussed as is the current state of knowledge regarding the mechanism of drug resistance. New insights into structure-function relationships in 4-aminoquinolines, both with respect to activity and resistance, are emphasised. Finally, patents registered since 1997 are described and an expert opinion offered. The review emphasises advances made during the last four years.

引用

页码：185 / 209

页数：25

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