Synthesis of 4-aminoquinoline–pyrimidine hybrids as potent antimalarials and their mode of action studies

One of the most viable options to tackle the growing resistance to the antimalarial drugs such as artemisinin is to resort to synthetic drugs. The multi-target strategy involving the use of hybrid drugs has shown promise. In line with this, new hybrids of quinoline with pyrimidine have been synthesi...

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Detalles Bibliográficos
Autores principales: Singh, Kamaljit, Kaur, Hardeep, Chibale, Kelly, Balzarini, Jan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Masson SAS. 2013
Materias:
Original Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7115683/
https://www.ncbi.nlm.nih.gov/pubmed/23811093
http://dx.doi.org/10.1016/j.ejmech.2013.05.046
Descripción
Sumario:One of the most viable options to tackle the growing resistance to the antimalarial drugs such as artemisinin is to resort to synthetic drugs. The multi-target strategy involving the use of hybrid drugs has shown promise. In line with this, new hybrids of quinoline with pyrimidine have been synthesized and evaluated for their antiplasmodial activity against both CQ(S) and CQ(R) strains of Plasmodium falciparum. These depicted activity in nanomolar range and were found to bind to heme as well as AT rich pUC18 DNA.

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