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Synthesis and characterization of sulphanilamide and benzimidazole pharmacophores containing γ-amino acid derivatives as dual antimicrobial and anticancer agents.

Authors :
Mackeviciute, Meta
Vaickelioniene, Rita
Anusevicius, Kazimieras
Siugzdaite, Jurate
Lelesius, Raimundas
Kavaliauskas, Povilas
Mickevicius, Vytautas
Source :
ARKIVOC: Online Journal of Organic Chemistry. 2023, Vol. 2023, p1-13. 13p.
Publication Year :
2023

Abstract

A series of γ-amino acid derivatives with sulfanilamide and benzimidazole pharmacophores in the structures were synthesized and evaluated for antibacterial and anticancer activity. Hydrazones with 5-nitrofur-2-yl and 5-nitrothien-2-yl moieties showed good inhibition against Staphylococcus aureus. Furthermore, hydrazones with a 5-nitrofur-2-yl moiety and a 2,5-dimethylpyrrole derivative demonstrated excellent inhibition of Listeria monocytogenes, which matched to control Cefazolin. Hydrazones bearing a 4-Me2NC6H4 fragment had a bactericidal effect against Escherichia coli two-fold stronger comparing to control. Hydrazones with 5-nitrofur-2-yl and 5-nitrothien-2-yl substituents were found to be the most active compounds against the Caco-2 colon adenocarcinoma cell line. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
15517004
Volume :
2023
Database :
Academic Search Index
Journal :
ARKIVOC: Online Journal of Organic Chemistry
Publication Type :
Academic Journal
Accession number :
175597972
Full Text :
https://doi.org/10.24820/ark.5550190.p012.015