Design and evaluation of novel antimalarial drugs

Antimalarial drugs

Description

Recent publications have identified a number of novel quinoline and acridone compounds that appear to either reverse or evade the chloroquine-resistance mechanism in vitro, and which are considered to be promising leads for the development of new antimalarials (Burgess et al. J Med Chem 2006; 49:5623-5, October et al. Chem Med Chem 2008; 3:1649-53, and Kelly et al. Nature 2009; 459:270-3). The efficacy of these compounds against chloroquine-resistant strains is thought to be due to their ability to block mutant PfCRT or, alternatively, to the absence of an interaction with PfCRT, which would allow the drugs to escape the resistance mechanism altogether.

We are designing and evaluating novel quinoline-type drugs, 'reversed-quinolines’, and 'resistance-reversers' in collaboration with a number of different groups including Dr Russell Barrow (ANU), Prof Tim Egan (University of Cape Town), Prof David Peyton (Portland State University and DesignMedix, Inc), Dr Jane Kelly and Prof Michael Riscoe (Portland VA Medical Center), Dr Christine Hrycyna and Prof Jean Chmielewski (Purdue University), and Dr Sandra Gemma and Prof Giuseppe Campiani (NatSynDrugs, University of Siena). The objective of this work is to test the ability of a range of novel drugs, reversed-quinolines, and resistance-reversers to interact with mutant PfCRT, and to provide insights into the structural features important for these interactions.

Recent papers from this project:

Selected media:

 
 
 
 
 
 
 
 
 

Partnerships

Dr Russell Barrow (ANU), Prof Tim Egan (University of Cape Town), Prof David Peyton (Portland State University and DesignMedix, Inc), Dr Jane Kelly and Prof Michael Riscoe (Portland VA Medical Center), Prof Jean Chmielewski (Purdue University), and Prof Giuseppe Campiani (NatSynDrugs, University of Siena).

 
 
 
 
 
 
 
 
 

Updated:  20 September 2017/Responsible Officer:  Director RSB/Page Contact:  Webmaster RSB