0000000000854881
AUTHOR
Yuris Popelis
Iron oxide superparamagnetic nanocarriers bearing amphiphilic N-heterocyclic choline analogues as potential antimicrobial agents
Magnetic nanoparticles represent an advanced tool in biomedicine because they can be simultaneously functionalized and guided using a magnetic field. Iron oxide magnetic nanoparticles precoated with oleic acid and bearing novel antimicrobial N-heterocyclic choline analogues, namely O-, N- and O,N-bis-undecyl-substituted N-(2-hydroxyethyl)-1,2,3,4-tetrahydroisoquinolinium derivatives, have been obtained as potential biomedical agents for drug delivery and antimicrobial therapy. Structural and size determinations for the novel synthesized magnetic nanosystems were carried out based upon magnetogranulometry, dynamic light-scattering measurements and X-ray diffraction analysis. The most expecte…
Synthesis and biological evaluation of lipid-like 5-(2-hydroxyethyl)-4-methyl-1,3-thiazole derivatives as potential anticancer and antimicrobial agents
A series of new lipid-like thiazole derivatives have been synthesized in good yields by O-alkylation of 5-(2-hydroxyethyl)-4-methyl-1,3-thiazole, a thiamine metabolite, under phase transfer catalysis conditions followed by N-alkylation with the aim to obtain potential anticancer and antimicrobial agents. The synthesized cationic amphiphiles and their ether precursors were subjected to in vitro cytotoxic evaluation against monolayer human fibrosarcoma HT-1080 and mouse hepatoma MG-22A tumour cell lines and normal mouse NIH 3T3 fibroblasts and were screened for antimicrobial activity concerning gram-positive and gram-negative bacterial and fungal strains. The synthesized compounds possessed s…
Silyl modification of biologically active compounds. 13. Synthesis, cytotoxicity and antibacterial action ofN-methyl-N-(2-triorganylsiloxyethyl)-1,2,3,4-tetrahydro(iso)quinolinium iodides
A series of N-methyl-N-(2-triorganylsiloxyethyl)-1,2,3,4-tetrahydro(iso)quinolinium iodides has been synthesized via dehydrocondensation reaction of N-(2-hydroxyethyl)-1,2,3,4-tetrahydroisoquinoline, N-(2-hydroxyethyl)-1,2,3,4-tetrahydroquinoline and 4,4-dimethyl-N-(2-hydroxyethyl)-4-sila-1,2,3,4-tetrahydroisoquinoline with trialkyl(aryl)hydrosilanes and subsequent alkylation, and characterized by 1H, 13C and 29Si NMR and mass spectroscopy. The biological activity data exhibited a marked enhancement of inhibitory activity against tumour cell lines and almost all the test bacterial/fungal strains in comparison with their 2-hydroxyethyl precursors. Cytotoxicity in the microgram range against …