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

被引：2

作者：

Sharma, Rupanjali ^{[1
]}

Goswami, Amrit ^{[2
]}

Rudrapal, Mithun ^{[1
]}

Sharma, Dipsikha ^{[1
]}

Sharma, Hemanta Kumar ^{[1
]}

Chetia, Dipak ^{[1
]}

机构：

[1] Dibrugarh Univ, Dept Pharmaceut Sci, Dibrugarh 786004, Assam, India

[2] North East Inst Sci & Technol, CSIR, Jorhat 785006, Assam, India

来源：

CURRENT SCIENCE | 2016年 / 111卷 / 12期

关键词：

Antimalarial; docking; HPLC; Plasmodium falcipurum; quinuclidine; mass; NMR; PLASMODIUM-FALCIPARUM; PLASMEPSIN-I; INHIBITORS;

D O I：

10.18520/cs/v111/i12/2028-2030

中图分类号：

O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];

学科分类号：

07 ; 0710 ; 09 ;

摘要：

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 mu g/ml) in comparison to chloroquine (EC50 5.144 mu 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.

引用

页码：2028 / 2030

页数：3

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