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Abstract
La resistencia desarrollada por el Plasmodium falciparum ante los fármacos tradicionales del tipo 4-amino-7-cloroquinolínicos ha llevado al diseño y síntesis de inhibidores duales, como los híbridos de la cloroquina. Además del farmacóforo típico en esta clase de antimaláricos, tales híbridos incorporan un espaciador metilénico como parte de un fragmento diamínico, cuyo propósito es la funcionalización del grupo amino terminal en sistemas heterocíclicos diversos con actividades biológicas reportadas. Esto con el fin de evitar la rápida eliminación de la molécula por parte del parásito, lo que se conoce como resistencia. Se discuten el diseño y síntesis de estos híbridos moleculares.
Palabras clave: Malaria, resistencia a la cloroquina, híbridos moleculares, funcionalización.
Abstract
Antimalarials: construction of molecular hybrids based on chloroquine. The resistance developed by Plasmodium falciparum against traditional 4-amino-7-chloro quinolinic 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.
Key words: malaria, chloro quine resistance, molecular hybrids, functionalization
Resumo
Antimaláricos: Construção de híbridos moleculares da cloroquina. A resistência desenvolvida pelo Plasmodium falciparum frente aos fármacos tradicionais do tipo 4-amino-7-cloroquinolínicos tem levado ao desenho e síntese de inibidores duais, como os híbridos da cloroquina. Além do farmacóforo típico nesta classe de antimaláricos, tais híbridos incorporam um espaçador metilénico como parte de um fragmento diamínico, que tem por propósito a funcionalização do grupo amino terminal em sistemas heterocíclicos diversos com atividades biológicas reportadas. Isto com a finalidade de evitar a rápida eliminação da molécula por parte do parasito, o que se conhece como resistência. É discutido o desenho e sínteses destes híbridos moleculares.
Palavras chave: Malária, resistência à cloroquina, híbridos moleculares, funcionalização
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