| Title |
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 |
| DOI |
10.24820/ark.5550190.p012.015 |
| Full Text |
|
| Is Part of |
Arkivoc.. Gainesville, FL : ARKAT USA. 2023, vol. 2023, iss. 7, p. 1-13.. ISSN 1551-7004. eISSN 1551-7012 |
| Keywords [eng] |
sulfanilamide ; benzimidazole ; γ-amino acids ; hydrazones ; azoles ; biological activity |
| Abstract [eng] |
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. |
| Published |
Gainesville, FL : ARKAT USA |
| Type |
Journal article |
| Language |
English |
| Publication date |
2023 |
| CC license |
|
