Publication: Next-Generation Antimalarial Drugs: Hybrid Molecules as a New Strategy in Drug Design
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2010
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2009 Wiley-Liss, Inc.
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Abstract
Malaria is a disease that affects nearly 40% of the global population, and chemotherapy
remains the mainstay of its control strategy. The global malaria situation is increasingly being exacerbated
by the emergence of drug resistance to most of the available antimalarials, necessitating search for novel
drugs. A recent rational approach of antimalarial drug design characterized as ‘‘covalent bitherapy’’
involves linking two molecules with individual intrinsic activity into a single agent, thus packaging dualactivity into a single hybrid molecule. Current research in this field seems to endorse hybrid molecules as
the next-generation antimalarial drugs. If the selective toxicity of hybrid prodrugs can be demonstrated in
vivo with good bioavailability at the target site in the parasite, it would offer various advantages including
dosage compliance, minimized toxicity, ability to design better drug combinations, and cheaper
preclinical evaluation while achieving the ultimate object of delaying or circumventing the development
of resistance. This review is focused on several hybrid molecules that have been developed, with particular
emphasis on those deemed to have high potential for development for clinical use. Drug Dev Res
71:20–32, 2010.
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malarial conjugates, trioxaquines and trioxolaquines, aminoquinolines, antimalarial resistance, malarial chemotherapy