• YAKHAK HOEJI
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• v.56 no.6
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• pp.390-394
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• 2012

A series of new pyridazinyl sulfoxides 3a~e and pyridazinyl sulfones 4a were synthesized for development of candidates to retain anticancer activity. The utility of sulfoxides and sulfones in both laboratory and industrial practice was quickly recognized, and these species have been extensively utilized, including as pharmaceutical intermediates and anticancer agents. Alkylthiopyridazines 2a~e were prepared from the 3,6-dichloropyridazine using allylthiolation with alkyl mercaptan. Sulfides could be oxidized to sulfoxides or sulfones using 1~3 equivalents of hydrogen peroxide as an oxidant. The oxidation of sulfoxides to sulfones was also accomplished with aqueous hydrogen peroxide. Formation of 3a~e and 4a was undertaken with stirring using 35% hydrogen peroxide at room temperature in acetic acid for 18~72 h. Synthetic compounds were identified using NMR spectrum.

• Bulletin of the Korean Chemical Society
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• v.29 no.11
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• pp.2291-2294
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• 2008

• Biomolecules & Therapeutics
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• v.14 no.4
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• pp.220-225
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• 2006

Derivatives of penicillanic acid sulfones are known to be irreversible inhibitors of $\beta$-lactamase. Eight 6-tricyclic methylene penicillanic acid sulfones were prepared, and their $\beta$-lactamase inhibitory activities were evaluated against $\beta$-lactamase types I, II, III and IV. Among the tricycles attached to 6-exomethylenepenam sulfones, thiazolobenzimidazole(12a-12b), fluorene(12c), and carbazole(12e), showed inhibitory activity on type I, II and III $\beta$-lactamase. But phenanthrene(12d), and anthracene(12f-12h) derivatives showed little $\beta$-lactamase inhibitory activity. The synergic effects of the selected compound(l2b) in 1:4 combination with piperacillin showed some protection to piperacillin for the resistant strains of E. coli DC2 and P. aeruginosa 1771.

• Bulletin of the Korean Chemical Society
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• v.33 no.10
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• pp.3175-3176
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• 2012

• Bulletin of the Korean Chemical Society
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• v.24 no.8
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• pp.1219-1222
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• 2003

• Bulletin of the Korean Chemical Society
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• v.31 no.7
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• pp.1887-1890
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• 2010

Cross-linked polystyrene supported aluminium triflate (Ps-Al(OTf)$_3$) was found to be an efficient and chemoselective heterogeneous Lewis acid catalyst for the direct conversion of arenes to sulfones using sulfonic acids as sulfonylating agents. The solid acid catalyst is stable (as a bench top catalyst) and can be easily recovered and reused without appreciable change in its efficiency.

• Bulletin of the Korean Chemical Society
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• v.10 no.4
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• pp.392-392
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• 1989

• Bulletin of the Korean Chemical Society
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• v.10 no.5
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• pp.482-483
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• 1989

• Bulletin of the Korean Chemical Society
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• v.31 no.8
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• pp.2337-2340
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• 2010

A series of new 6-aryl-3-(3,4-dimethoxy-phenyl)-2-phenylsulfanyl-imidazo[2,1-b]-thiazole (5a-c) and 6-aryl-2-benzenesulfonyl-3-(3,4-dimethoxy-phenyl)imidazo[2,1-b]- thiazole (6a-c) have been prepared and characterized by analytical and spectral methods. The title compounds 5a-c and 6a-c were obtained by the reaction of 4-(3,4-dimethoxy-phenyl)-5-phenylsulfanyl-thiazol-2-ylamine (3) and 5-benzenesulfonyl-4-(3,4-dimethoxy -phenyl)thiazol-2-ylamine (4) with various phenacyl bromides in anhydrous ethanol. These newly synthesized compounds (5a-c and 6a-c) were screened for their anthelmintic and anti-inflammatory activities, where they have displayed better activities.

• YAKHAK HOEJI
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• v.51 no.6
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• pp.447-454
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• 2007

The resistance of bacteria against ${\beta}$-lactam antibiotics is mainly caused by the production of ${\beta}$-lactamase enzymes. ${\beta}$-Lactamase inhibitors are used in combination with known antibiotics to overcome the growing problem of bacterial resistance. We prepared 6-(thienylmethylene)penam sulfones for the development of potent ${\beta}$-lactamase inhibitors and evaluated their ${\beta}$-lactamase inhibitory activities.