Universitas Scientiarum (Dec 2008)
Antimaláricos: construcción de híbridos moleculares de la cloroquina
Abstract
Antimalarials: construction of molecular hybrids based on chloroquine. The resistance developed by Plasmodium falciparum againsttraditional 4-amino-7-chloroquinolinic drugs has lead to the design and synthesis of dual inhibitors such as chloroquine hybrids. Besidesthe usual pharmacophore in this type of antimalarials, such hybrids incorporate a methylenic spacer as part of a diaminic fragment whosepurpose is the functionalization of the terminal amino group in various heterocyclic systems having reported biological activities. The primegoal is to avoid the molecule rapid elimination by the parasite, which is known as resistance. The design and synthesis of these molecularhybrids are discussed.