2020
DOI: 10.1002/ardp.202000277
|View full text |Cite
|
Sign up to set email alerts
|

Synthesis, antimicrobial evaluation, DNA gyrase inhibition, and in silico pharmacokinetic studies of novel quinoline derivatives

Abstract: Herein, we report the synthesis and in vitro antimicrobial evaluation of novel quinoline derivatives as DNA gyrase inhibitors. The preliminary antimicrobial activity was assessed against a panel of pathogenic microbes including Gram‐positive bacteria (Streptococcus pneumoniae and Bacillus subtilis), Gram‐negative bacteria (Pseudomonas aeruginosa and Escherichia coli), and fungal strains (Aspergillus fumigatus, Syncephalastrum racemosum, Geotrichum candidum, and Candida albicans). Compounds that revealed the be… Show more

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...
3
1
1

Citation Types

0
21
0

Year Published

2021
2021
2023
2023

Publication Types

Select...
7

Relationship

4
3

Authors

Journals

citations
Cited by 37 publications
(22 citation statements)
references
References 38 publications
0
21
0
Order By: Relevance
“…Quinoline belongs to a biologically active class of compounds as they show quite diverse biological activities [ 6 ]. Many scientific reports revealed that natural and synthetic quinolines are drawn considerable attention in medicinal chemistry [ 7 , 8 ]. The great attention paid by researchers to the study of quinoline derivatives is explained by their broad range of biological activities, such as anti-Alzheimer [ 9 ], antidiabetic [ 10 ], anti-inflammatory [ 11 ], antituberculosis [ 12 ], anticancer [ 13 ], antioxidant [ 14 ], and as inhibitors of SARS‐CoV‐2 (COVID-19) virus [ 15 – 17 ].…”
Section: Introductionmentioning
confidence: 99%
“…Quinoline belongs to a biologically active class of compounds as they show quite diverse biological activities [ 6 ]. Many scientific reports revealed that natural and synthetic quinolines are drawn considerable attention in medicinal chemistry [ 7 , 8 ]. The great attention paid by researchers to the study of quinoline derivatives is explained by their broad range of biological activities, such as anti-Alzheimer [ 9 ], antidiabetic [ 10 ], anti-inflammatory [ 11 ], antituberculosis [ 12 ], anticancer [ 13 ], antioxidant [ 14 ], and as inhibitors of SARS‐CoV‐2 (COVID-19) virus [ 15 – 17 ].…”
Section: Introductionmentioning
confidence: 99%
“…The ester derivatives ( 4 – 6 ) were readily obtained by reacting the potassium salt 3 a under reflux with the appropriate α‐chloroester derivative. [ 49–54 ] However, α‐chloroacetyl chloride was allowed to react with a variety of aromatic amines to obtain the corresponding α‐chloro‐ N ‐arylamides. [ 35,55 ] Treating the potassium salt of 3 a with the freshly prepared α‐chloro‐ N ‐arylamides furnished the corresponding amide derivatives 7 – 14 .…”
Section: Resultsmentioning
confidence: 99%
“…[35][36][37] The resulting N 1 -ethylbenzene-1,2-diamine was utilized for the preparation of 1-ethylquinoxaline-2,3(1H,4H)-dione through condensation with diethyl oxalate. [38] Treatment of the latter with hydrazine hydrate in refluxing ethanol [39,40] readily afforded 1-ethyl-3hydrazinylquinoxalin-2(1H)-one (17). [34] As depicted in Schemes 2 and 3, compound 17 was used as a starting material for the synthesis of both new sets of target compounds.…”
Section: Chemistrymentioning
confidence: 99%