Current Science

Rupanjali Sharma ¹, Amrit Goswami ², Mithun Rudrapal ¹, Dipsikha Sharma ¹, Hemanta Kumar Sharma ¹, Dipak Chetia ¹

Affiliations
1 Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugarh 786 004, IN
2 CSIR-North East Institute of Science and Technology, Jorhat 785 006, IN

Abstract

A simple Schiff base, N-(pyridine-4-yl-methylene) quinuclidine-3-amine was synthesized from 3-amino-quinuclidine and 4-pyridine carboxaldehyde. The physico-chemical properties of the synthesized com-pound 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 μg/ml) in comparison to chloroquine (EC₅₀ 5.144 μg/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.

Keywords

Antimalarial, Docking, HPLC, Plasmodium falcipurum, Quinuclidine, Mass, NMR.

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