Abstract

KOUZNETSOV, Vladímir V.  and  AMADO TORRES, Diego F.. Antimalarials: construction of molecular hybrids based on chloroquine. Univ. Sci. [online]. 2008, vol.13, n.3, pp.306-320. ISSN 0122-7483.

The resistance developed by Plasmodium falciparum against traditional 4-amino-7-chloroquinolinic drugs has lead to the design and synthesis of dual inhibitors such as chloroquine hybrids. Besides the usual pharmacophore in this type of antimalarials, such hybrids incorporate a methylenic spacer as part of a diaminic fragment whose purpose is the functionalization of the terminal amino group in various heterocyclic systems having reported biological activities. The prime goal is to avoid the molecule rapid elimination by the parasite, which is known as resistance. The design and synthesis of these molecular hybrids are discussed.

Keywords : malaria; chloroquine resistance; molecular hybrids; functionalization.

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