Synthesis of Some 4-Quinolones and Related Structures for Evaluation as Potential Anti-Malarial Agents.

摘要

The need for effective prophylactic agents in plasmodial infections in humans made it desirable to explore the antimalarial effect of a series of compounds chemically related to endochin (2-methyl-3-n-heptyl-7-methoxy-4(1H)-quinolone). The authors have synthesized and submitted for prophylactic as well as therapeutic antimalarial evaluation some new 4(1H)-quinolones and 4-hydroxyl-l, 5-naphthyridines,all related to endochin but whose structures were sufficiently modified to incorporate the present knowledge as to the nature and position of substituents more likely to enhance antiplasmodial activity. Also several materials prepared either as intermediates or as model compounds in the synthetic work were submitted for evaluation. Compounds were evaluated in the P. berghei test system in mice for effectiveness and toxicity.