Antiprotozoals based on the inhibition of N-Myristoyltransferase

Abstract

The research performed a protozoal structure activity investigation based on the transition state of N-Myristoyltransferase. This initial investigation synthesised a simplified transition state mimetic based from myristic acid and included alkene and phenoxy variation of the myristoyl chain. A series of Inhibitors were developed using a coenzyme-A fragment. Structures were targeted that were based on the statins (HMG-CoA inhibitors). Some of the compounds developed showed micro molar activities towards T. brucei and P. falciparum.