Application of multicomponent reactions to antimalarial drug discovery. Part 3: discovery of aminoxazole 4-aminoquinolines with potent antiplasmodial activity in vitro

Chitalu C Musonda; Susan Little; Vanessa Yardley; Kelly Chibale

doi:10.1016/j.bmcl.2007.06.070

Application of multicomponent reactions to antimalarial drug discovery. Part 3: discovery of aminoxazole 4-aminoquinolines with potent antiplasmodial activity in vitro

Bioorg Med Chem Lett. 2007 Sep 1;17(17):4733-6. doi: 10.1016/j.bmcl.2007.06.070. Epub 2007 Jun 27.

Authors

Chitalu C Musonda¹, Susan Little, Vanessa Yardley, Kelly Chibale

Affiliation

¹ Department of Chemistry, University of Cape Town, Rondebosch, South Africa.

PMID: 17644333
DOI: 10.1016/j.bmcl.2007.06.070

Abstract

The synthesis and antimalarial activity of a novel series of first generation 4-aminoquinoline-containing 2,4,5-trisubstituted aminoxazoles against two strains of the Plasmodium falciparum parasite in vitro is described. A number of compounds significantly more potent than the standard drug chloroquine were identified.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Aminoquinolines / chemistry*
Animals
Antimalarials / chemical synthesis*
Antimalarials / pharmacology*
Chemistry, Pharmaceutical / methods*
Drug Design
Drug Evaluation, Preclinical
Inhibitory Concentration 50
Oxazoles / chemistry*
Parasitic Sensitivity Tests
Plasmodium / metabolism
Plasmodium falciparum / drug effects*
Structure-Activity Relationship

Substances

Aminoquinolines
Antimalarials
Oxazoles
4-aminoquinoline