β-amino-alcohol tethered 4-aminoquinoline-isatin conjugates: Synthesis and antimalarial evaluation

A series of β-amino alcohol tethered 4-aminoquinoline-isatin conjugates were synthesized with the aim of probing their antimalarial structure activity relationship. Two of the most active conjugates (11b and 11f) exhibited antimalarial efficacy comparable to that of chloroquine, with IC(50) values o...

Descripción completa

Detalles Bibliográficos
Autores principales: Nisha, Gut, Jiri, Rosenthal, Philip J., Kumar, Vipan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Masson SAS. 2014
Materias:
Short Communication
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7115587/
https://www.ncbi.nlm.nih.gov/pubmed/25062007
http://dx.doi.org/10.1016/j.ejmech.2014.07.064
Descripción
Sumario:A series of β-amino alcohol tethered 4-aminoquinoline-isatin conjugates were synthesized with the aim of probing their antimalarial structure activity relationship. Two of the most active conjugates (11b and 11f) exhibited antimalarial efficacy comparable to that of chloroquine, with IC(50) values of 11.8 and 13.5 nM, respectively against chloroquine resistant W2 strain of Plasmodium falciparum and are devoid of any cytotoxicity.

Ejemplares similares