• Bulletin of the Korean Chemical Society
• /
• v.26 no.5
• /
• pp.833-836
• /
• 2005

• Bulletin of the Korean Chemical Society
• /
• v.29 no.4
• /
• pp.723-724
• /
• 2008

• Bulletin of the Korean Chemical Society
• /
• v.31 no.7
• /
• pp.1843-1847
• /
• 2010

An efficient method for the preparation of 1,4-disubstituted 1,2,3-triazole compounds is described using polymeric quaternary ammonium salts having azide or alkyne functionality to remove unreacted excess starting molecules (azide/alkyne). Copper metal could easily be removed by simple filtration with a short $Na_2SO_4$/silica cartridge, affording highly regioselective products in high yield and excellent purity without the need for work-up, extraction and chromatographic purification.

• Journal of the Korean Chemical Society
• /
• v.54 no.6
• /
• pp.731-736
• /
• 2010

Several new 5-aryl-3-($\beta$-D-glucopyranosylthio)-1,2,4-triazoles have been synthesized. The structures of these new compounds were confirmed by $^1H$ NMR, $^{13}C$ NMR and elemental analyses.The antibacterial activities of the compounds were also evaluated.

• Archives of Pharmacal Research
• /
• v.13 no.2
• /
• pp.142-146
• /
• 1990

Reaction of ethyl 4-chloro-2-phenylpyrimidine-4-carboxylate (4) with 5-chloro-2-methylthiophenol or 3-aryl-4-phenyl-1, 2, 4-triazole-5 thiol yielded the corresponding thioethers (5) and (8a, b), respectively. Careful alkaline hydrolysis of (5) yielded the corresponding carboxylic acid (6). Reaction of (4) with p-aminoacetophenone yielded compound (10) which was reacted with certain aromatic aldehyde to afford the$\alpha,\beta$-unsaturated ketones (11a-d). Condensation of (11a-d) with malononitrile or phenylhydrazine yielded the 2-amino-3-cyanopyridines (12a-f) or the 2-pyrazolines (13a, b) respectively. Seven representative compounds were tested for their in vitro antimicrobial activity against some pathogenic micro-organisms, some of them were proved to be active.

• Bulletin of the Korean Chemical Society
• /
• v.26 no.11
• /
• pp.1790-1794
• /
• 2005

Fréchet-type dendritic benzyl azides were efficiently synthesized using 5-(azidomethyl)-1,3-dihydroxybenzene as an azide focal point functionalized unit by adding a generation to the existing dendron and applied for the construction of dendrimers containing 1,2,3-triazole rings as connectors via click chemistry with a tripodal acetylene core.

• Bulletin of the Korean Chemical Society
• /
• v.32 no.8
• /
• pp.2657-2660
• /
• 2011

1,2,4-Triazoles and quinoxalines were found to display various pharmacological activities. Hence a series of 1-aryl-4-methyl-1,2,4-triazolo[4,3-a]quinoxalines were synthesized. Due to various advantages of organic reactions under solvent-free conditions these compounds were developed using iodobenzene diacetate under solvent-free conditions. The synthesized compounds were characterized by elemental microanalysis, infrared spectroscopy, $^1H$ NMR, $^{13}C$ NMR and HRMS. All the synthesized compounds were investigated for their antitubercular activity and 5g was found to the most active compound.

• Archives of Pharmacal Research
• /
• v.28 no.4
• /
• pp.438-442
• /
• 2005

A series of 3-[1-(4-(2-methylpropyl) phenyl) ethyl]-1,2,4-triazole-5-thione (I) and its bicyclic condensed derivatives 6-benzylidenethiazolo[3,2-b]-1, 2,4-triazole-5(6H)-ones (IIa-IIf) were investigated for the prevention of ethanol-induced oxidative stress in liver and brain of mice. Administration of ethanol (0.1 mL/mice, p.o.) resulted in a drop of total thiol groups (T-SH) and non-protein thiol groups (NP-SH), and an increase in thiobarbituric acid reactive substances (TBARS) in both liver and brain tissue of mice (p<0.001). Among the compounds investigated (at a dose of 200 mg/kg, p.o.), I and IId ameliorated the peroxidative injury in these tissues effectively. Compounds IIa, IIc and IIe improved the peroxidative tissue injury only in brain. These findings suggest that certain condensed thiazolo-triazole compounds may contribute to the control of ethanol-induced oxidative stress in an organ selective manner.

• Bulletin of the Korean Chemical Society
• /
• v.29 no.8
• /
• pp.1561-1564
• /
• 2008

Although the use of Cu(II) salts as catalysts without reductants is limited in the cycloaddition of acetylenes with azides, the catalytic system employing average 10 nm CuO(II) nanoparticles in the absence of reductants shows good catalytic activity to form 1,4-disubstituted 1,2,3-triazoles even in wet THF as well as water. It is also noticeable that CuO(II) nanoparticle catalysts can be recycled with consistent activity. A range of alkynes and azides were subject to the optimized CuO(II) nanoparticle-catalyzed cycloaddition reaction conditions to afford the desired products in good yields.

• Parasites, Hosts and Diseases
• /
• v.55 no.6
• /
• pp.661-665
• /
• 2017

We synthesized C-10 substituted triazolyl artemisinins by the Huisgen cycloaddition reaction between dihydroartemisinins (2) and variously substituted 1, 2, 3-triazoles (8a-8h). The antimalarial activities of 32 novel artemisinin derivatives were screened against a chloroquine-resistant parasite. Among them, triazolyl artemisinins with electron-withdrawing groups showed stronger antimalarial activities than those shown by the derivatives having electron-donating groups. In particularly, m-chlorotriazolyl artemisinin (9d-12d) showed antimalarial activity equivalent to that of artemisinin and could be a strong drug candidate.