SYNTHESIS AND ANTIMALARIAL ACTIVITY OF SOME NEOCRYPTOLEPINE ANALOGUES CARRYING A MULTIFUNCTIONAL LINEAR AND BRANCHED CARBON-SIDE CHAINS

摘要

The synthesis and in vitro antimalarial activity of several neocryptolepine analogues carrying either a linear or branched dibasic side chain at C11 are described. Many of these neocryptolepine analogues have low nanomolar antimalarial activity against the chloroquine-sensitive P. falciparum strain (NF54). The data also demonstrated that a branched structural motif is not superior for antimalarial activity over a linear side chain, but their thioureido derivatives showed lower cytotoxicity than the linear one. Ureido and thioureido derivatives also showed stronger β-haematin inhibition than the corresponding free amines.