Werbovetz Karl
The Ohio State University, Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, Columbus 43210-1291, USA.
Curr Opin Investig Drugs. 2006 Feb;7(2):147-57.
Diamidine-containing compounds have a long history of use in the treatment of African trypanosomiasis and leishmaniasis. The discovery that diamidine prodrugs possess in vivo antimicrobial activity when administered orally has led to a renewed interest in this class of compounds for the treatment of parasitic infections. In this review, the selectivity of diamidines against trypanosomes, Leishmania and Plasmodium is rationalized through mechanism-of-action studies. An overview of the antiprotozoal activities of newer diamidines and diamidine prodrugs is also presented, along with a summary of the progress made toward the clinical development of new diamidines for use against these parasitic diseases.
含脒化合物在治疗非洲锥虫病和利什曼病方面有着悠久的使用历史。口服给药时，脒前药具有体内抗菌活性这一发现，引发了人们对这类化合物治疗寄生虫感染的新兴趣。在本综述中，通过作用机制研究，阐述了脒对锥虫、利什曼原虫和疟原虫的选择性。还概述了新型脒和脒前药的抗原虫活性，以及新型脒用于治疗这些寄生虫病的临床开发进展总结。
