Design and Synthesis of Brain Penetrant Trypanocidal N-Myristoyltransferase Inhibitors

J Med Chem. 2017 Dec 14;60(23):9790-9806. doi: 10.1021/acs.jmedchem.7b01255.

Tracy Bayliss ¹, David A Robinson ¹, Victoria C Smith ¹, Stephen Brand ¹, Stuart P McElroy ¹, Leah S Torrie ¹, Chido Mpamhanga ¹, Suzanne Norval ¹, Laste Stojanovski ¹, Ruth Brenk ¹, Julie A Frearson ¹, Kevin D Read ¹, Ian H Gilbert ¹, Paul G Wyatt ¹

Affiliations

Affiliation

1 Drug Discovery Unit, College of Life Sciences, University of Dundee , Sir James Black Centre, Dundee DD1 5EH, U.K.

PMID: 29125744 DOI: 10.1021/acs.jmedchem.7b01255

Abstract

N-myristoyltransferase (NMT) represents a promising drug target within the parasitic protozoa Trypanosoma brucei (T. brucei), the causative agent for human African trypanosomiasis (HAT) or sleeping sickness. We have previously validated T. brucei NMT as a promising druggable target for the treatment of HAT in both stages 1 and 2 of the disease. We report on the use of the previously reported DDD85646 (1) as a starting point for the design of a class of potent, brain penetrant inhibitors of T. brucei NMT.

Name
Email *

	Sorry, but the email address you supplied was invalid.