Antimalarial polyamine analogs

ML Edwards, DM Stemerick, AJ Bitonti…

Index: Edwards, M. L.; Stemeric, D. M.; Bitonti, A. J.; Dumont, J. A.; McCann, P. P.; et al. Journal of Medicinal Chemistry, 1991 , vol. 34, # 2 p. 569 - 574

Full Text: HTML

Citation Number: 47

Abstract

A series of novel tetraamines of the general formula RNH (CHz), NH (CHz), NH (CHz) zNHR was synthesized and examined for activity against growth of Plasmodium falciparum in vitro. Within the series, dibenzyl analogues (R= benzyl) were found to be the most effective growth inhibitors, with ICw values of about lo4 M. Further modifications of the tetraamine provided the optimum chain length for antimalarial activity of y= 7, x= 3. Compound 8 (MDL 27,695) ...