Work

Parallel Synthesis and Antimalarial Screening of a 4-Aminoquinoline Library

Year: 2004

Type: article

Abstract: Due to growing problems with drug resistance, there is an outstanding need for new, cost-effective drugs for the treatment of malaria. The 4-aminoquinolines have provided a number of useful antimalarials, and Plasmodium falciparum, the causative organism for the most deadly form of human malaria, is generally slow to develop resistance to these drugs. Therefore, diverse screening libraries of quinolines continue to be useful for antimalarial drug discovery. We report herein the development of an efficient method for producing libraries of 4-aminoquinolines variant in the side chain portion of the molecule. The effects of these substitutions were evaluated by screening this library for activity against P. falciparum, revealing four potent compounds active against drug-resistant strains.

Source: Journal of Combinatorial Chemistry

DOI: 10.1021/cc0340473

Authors: Peter B. Madrid, Nathan T. Wilson, Joseph L. DeRisi, R. Kiplin Guy

Institution: University of California, San Francisco

Language: English

Topic: Malaria Research and Control

Subfield: Public Health, Environmental and Occupational Health

Field: Medicine

Domain: Health Sciences

SDG: Good health and well-being

Open Access status: green

Funder: National Institute of Allergy and Infectious Diseases