Synthesis and evaluation of chirally defined side chain variants of 7-chloro-4-aminoquinoline to overcome drug resistance in malaria chemotherapy. [PublishAheadOfPrint]

A novel 4-aminoquinoline derivative ((S)-7-chloro-N-(4-methyl-1-(4-methylpiperazin-1-yl)pentan-2-yl)-quinolin-4-amine triphosphate) exhibiting curative activity against chloroquine resistant malaria parasite has been identified for preclinical development as a blood schizonticidal agent. The lead molecule selected after detailed SAR studies, has good solid state properties, and has promising activity against in vitro and in vivo experimental malaria models. The in vitro ADME parameters have indicated favourable drug like profile.

http://ift.tt/2hog8sS