3 research outputs found
Synthesis and antimalarial activity of novel N-{2-[2-(2-aminoethoxy) ethoxy] ethyl}-7-chloroquinolin-4-amine and its derivatives
233-241A number of N-{2-[2-(2-aminoethoxy)ethoxy]ethyl}-7-chloroquinolin-4-amine
derivatives have been prepared by condensation of N-{2-[2-(2-aminoethoxy)
ethoxy] ethyl}-7-chloroquinolin-4-amine with substituted aldehyde. The newly
synthesized compounds have been characterized by IR, ¹H and ¹³C NMR, and mass
spectral data. These compounds have been screened for in vitro antimalarial activity using the Sybr Green assay of P. falciparum in culture and the heme
detoxification based Heme-HRP assay. Among these, compounds
7-chloro-N-[2-(2-{2-[(2, 4-difluorobenzyl) amino] ethoxy} ethoxy) ethyl]
quinolin-4-amine is found to be
the most effective with IC50 value 60 M (in Heme-HRP assay) and 48
nM (in P. falciparum culture assay). These values compare well with the
potency of chloroquine in the respective assays