Antioxidant and Antimicrobial Potential of 1,8-Naphthyridine Based Scaffolds: Design, Synthesis and in Silico Simulation Studies within Topoisomerase II.
Chem Biodivers
; 21(6): e202301746, 2024 Jun.
Article
in En
| MEDLINE
| ID: mdl-38459958
ABSTRACT
A series of spiro ß-Lactams (4 a-c, 7 a-c) and thiazolidinones (5 a-c, 8 a-c) possessing 1,8-naphthyridine moiety were synthesized in this study. The structure of the newly synthesized compounds has been confirmed by IR, 1H-NMR, 13Câ
NMR, mass spectra, and elemental analysis. The synthesized compounds were tested inâ
vitro for their antibacterial and antifungal activity against various strains. The antimicrobial data showed that most of the compounds displayed good efficacy against both bacteria and fungi. The structure-activity relationship (SAR) studies suggested that the presence of electron-withdrawing chloro (3 b, 4 b, and 5 b) and nitro groups (7 b, 8 b) at the para position of the phenyl ring improved the antimicrobial activity of the compounds. The free radical scavenging assay showed that all the synthesized compounds exhibited significant antioxidant activity on DPPH. Compounds 8 b (IC50=17.68±0.76â
µg/mL) and 4 c (IC50=18.53±0.52â
µg/mL) showed the highest antioxidant activity compared to ascorbic acid (IC50=15.16±0.43â
µg/mL). Molecular docking studies were also conducted to support the antimicrobial and SAR results.
Key words
Full text:
1
Database:
MEDLINE
Main subject:
Drug Design
/
Microbial Sensitivity Tests
/
DNA Topoisomerases, Type II
/
Fungi
/
Anti-Bacterial Agents
/
Antifungal Agents
/
Naphthyridines
/
Antioxidants
Language:
En
Journal:
Chem Biodivers
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2024
Type:
Article
Affiliation country:
Saudi Arabia