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No presente trabalho realizou-se a sintese de novos N-derivados da 4-amino-7-cloroquinolina modificando seletivamente o grupo amino terminal das N-(7-cloroquinolin-4-il)-alquildiaminas, a base do farmaco cloroquina (CQ) mediante a incorporacao de sistemas heterociclicos da 2-imino-tiazolidin-4-ona e 1H-pirrol-2,5-diona. Esses derivados foram selecionados gracas as suas propriedades caracteristicas, e avaliados mediante crivado virtual empregando as plataformas OSIRIS e Molinspiration. Os derivados quinolinicos assim desenhados e sintetizados poderiam incrementar a atividade antimalarica dos analogos da CQ sem afetar a lipofilia como tem se descrito na literatura, postulando-se como candidatos em posteriores testes biologicos. In the present work, the syntheses of new 4-amino-7-chloroquinoline N-derivatives were performed by selective modification of the side chain amino group of N-(7-chloroquinolin-4-yl) alkyldiamines, basis framework of chloroquine (CQ) drug through the incorporation of heterocyclic 2-imino-thiazolidin-4-one and 1H-pyrrol-2,5-dione systems. These potential activity modulators were selected thanks to their characteristic properties, and evaluated by virtual screening employing the OSIRIS and Molinspirations platforms. Designed and synthesized quinolinic derivatives could increase the antimalarial activity of CQ analogues without affecting the lipophilicity as described in literature, suggesting them as candidates for further biological assessments.

journal of the brazilian chemical society

Property-based design and synthesis of new chloroquine hybrids via simple incorporation of 2-imino-thiazolidin-4-one or 1h-pyrrol-2, 5-dione fragments on the 4-amino-7-chloroquinoline side chain