Quinoline: A Promising Scaffold in Recent Antiprotozoal Drug Discovery

摘要

Protozoal infections malaria and leishmania have become most prevalent in recent times. A high death rate is reported world- wide because of these diseases. Although there are only a few antiprotozoal drugs but could not be used anymore to cure protozoal diseases because of their toxic effects. Despite the non-ceasing attempts to discover the drugs to cure malaria and leishmania, efficient drug-design with low toxicity could not be achieved. A wide range of heterocyclic pharmacophores have been utilized to design efficient drugs. Amongst these hetero- cycles, quinoline bicycle is given a high priority, since a vast literature of quinoline derivatives relevant to potent pharmaco- logical properties is available. The efficacy of the drugs lies upon the good bioavailability, favorable pharmacokinetics, and pharmacodynamics of the molecule. In view of these, the continual efforts are being put to bring about potent anti- protozoal agents to clinical stage. In this review, the potential research done recently towards the anti-protozoal drug-design and discovery is compiled comprehensively. The importance of structural features attributed to remarkable activity is described taking consideration of structure-activity relationship. Safety Index (SI), crucial for clinical efficiency of a drug is compared amongst a set of derivatives which involve inhibitory proper- ties, in addition to the cytotoxic effects.