New amine and urea analogs of ferrochloroquine: synthesis, antimalarial activity in vitro and electrochemical studies

被引：74

作者：

Chibale, K ^{[1
]}

Moss, JR

Blackie, M

van Schalkwyk, D

Smith, PJ

机构：

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

[2] Univ Cape Town, Dept Pharmacol, ZA-7925 Cape Town, South Africa

来源：

TETRAHEDRON LETTERS | 2000年 / 41卷 / 32期

基金：

新加坡国家研究基金会; 英国惠康基金;

关键词：

D O I：

10.1016/S0040-4039(00)01036-4

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Amine and urea analogs of ferrochloroquine with varying methylene spacer lengths were synthesised, studied by cyclic voltammetry and evaluated in vitro against a sensitive (D10) and resistant (K1) strain of Plasmodium falciparum. Most analogs were found to be more active than chloroquine in both strains. In D10 ureas were more active than amines and antimalarial activity in this strain correlated well with the length of the methylene spacer and redox potentials. The length of the methylene spacer was a major determinant of antimalarial activity in K1. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：6231 / 6235

页数：5

共 9 条

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