In vitro evaluation of the antimalarial activity of a designed novel quinuclidine derivative

نویسندگان

  • Rupanjali Sharma
  • Amrit Goswami
  • Mithun Rudrapal
  • Dipsikha Sharma
  • Hemanta Kumar Sharma
  • Dipak Chetia
چکیده

A simple Schiff base, N-(pyridine-4-yl-methylene) quinuclidine-3-amine was synthesized from 3-aminoquinuclidine and 4-pyridine carboxaldehyde. The physico-chemical properties of the synthesized compound were studied. Molecular docking study was carried out and the quinuclidine derivative was evaluated for its in vitro antimalarial activity against chloroquine-sensitive Plasmodium falciparum strain. Although higher dose of synthesized compound was required for antimalarial activity (EC50 = 13.125 g/ml) in comparison to chloroquine (EC50 5.144 g/ml), the correlation coefficient confirmed good fit of the data. Furthermore, the result of the molecular docking provided insights into the ligand–protein interactions responsible for the inhibitory potency.

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تاریخ انتشار 2016