2016
DOI: 10.18520/cs/v111/i12/2028-2030
|View full text |Cite
|
Sign up to set email alerts
|

<i>In Vitro</i> Evaluation of the Antimalarial Activity of a Designed Novel Quinuclidine Derivative

Abstract: 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 (EC 50 = 13.125 g/ml) in com… Show more

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...
3
1
1

Citation Types

0
5
0

Year Published

2018
2018
2022
2022

Publication Types

Select...
7

Relationship

1
6

Authors

Journals

citations
Cited by 7 publications
(5 citation statements)
references
References 12 publications
0
5
0
Order By: Relevance
“…Molecular docking studies are usually performed on free like AutoDock (Art Olsen, David Goodsell, Scripps), and commercial software packages such as Discovery Studio (Accelrys), Glide (Schrodinger), GOLD (CCDC) and FlexX (BiosolveIT). The crystal structures of protein molecules of interest are retrieved from the RCSB Protein Data Bank (https://www.rcsb.org) 31,32 . The methodology involved in molecular docking is depicted in Figure 4.…”
Section: Docking Methodologymentioning
confidence: 99%
“…Molecular docking studies are usually performed on free like AutoDock (Art Olsen, David Goodsell, Scripps), and commercial software packages such as Discovery Studio (Accelrys), Glide (Schrodinger), GOLD (CCDC) and FlexX (BiosolveIT). The crystal structures of protein molecules of interest are retrieved from the RCSB Protein Data Bank (https://www.rcsb.org) 31,32 . The methodology involved in molecular docking is depicted in Figure 4.…”
Section: Docking Methodologymentioning
confidence: 99%
“…21,22,23 Two strains were used for the study, one is CQ-sensitive 3D-7 and the other is CQ-resistant RKL-2. All the test compounds, 4a-j were initially screened at two fixed doses, 5 µg/ml and 50 µg/ml against CQ-sensitive strain.…”
Section: Antimalarial Activity Evaluationmentioning
confidence: 99%
“…Schiff base, which was named after Hugo Schiff [1], was prepared via condensation reaction between amino functionality and an aldehydic/ketonic carbonyl [2]. The medicinal potential of Schiff bases in drug designed is quite evident in their reported diverse pharmacological properties which include antimicrobial [3], anticancer [4], antitumor [5], anti-convulsant [6], antimalarial [7], antitubercular [8], anti-HIV, anti-inflammatory [9], antidepressant activities among others [10]. Their enhanced reported bioactivity might be as a result of their improved lipophilic character thereby improving their bioavailability in the lipid membranes; therefore, resulting in growth redundancy in the organism [11].…”
Section: Introductionmentioning
confidence: 99%