O'Neill Paul M, Ward Stephen A, Berry Neil G, Jeyadevan J Prince, Biagini Giancarlo A, Asadollaly Egbaleh, Park B Kevin, Bray Patrick G
Department of Pharmacology and Therapeutics, University of Liverpool, Liverpool L67 7ZD UK.
Curr Top Med Chem. 2006;6(5):479-507. doi: 10.2174/156802606776743147.
A broad overview is presented describing the current knowledge and the ongoing research concerning the 4-aminoquinolines (4AQ) as chemotherapeutic antimalarial agents. Included are discussions of mechanism of action, structure activity relationships (SAR), chemistry, metabolism and toxicity and parasite resistance mechanisms. In discussions of SAR, particular emphasis has been given to activity versus chloroquine resistant strains of Plasmodium falciparum. Promising new lead compounds undergoing development are described and an overview of physicochemical properties of chloroquine and amodiaquine analogues is also included.
本文提供了一个广泛的概述，描述了关于4-氨基喹啉（4AQ）作为抗疟化疗药物的当前知识和正在进行的研究。内容包括作用机制、构效关系（SAR）、化学、代谢、毒性以及寄生虫耐药机制的讨论。在构效关系的讨论中，特别强调了对恶性疟原虫氯喹耐药菌株的活性。描述了正在开发的有前景的新先导化合物，并概述了氯喹和阿莫地喹类似物的物理化学性质。
