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Abstract
Quinoline antimalarial patents and relevant scientific literature concerning their mechanism of action, mechanism of resistance and structure-function relationships are discussed in this review. The review provides a brief history of current antimalarial drugs and describes some salient features about their use, occurrence of drug resistance, their metabolism and known adverse effects. Recent advances in our understanding of the mechanism of action of 4-aminoquinolines, quinoline methanols and 8-aminoquinolines are discussed as is the current state of knowledge regarding the mechanisms of drug resistance. New insights into structure-function relationships in 4-aminoquinolines, both with respect to activity and resistance, are emphasised. Finally, patents registered since 1997 are described and an expert opinion offered. The review emphasises advances made during the last four years.