• YAKHAK HOEJI
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• v.46 no.2
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• pp.89-92
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• 2002

Allylthio group of the sulfur compounds of garlic oil plays an important role for prevention and treatment of hepatic diseases induced by toxic substances or carbon tetrachloride. Thus allylthio group as pharmacologically active group was introduced into pyridazine heterocycle ring. Aryloxyallylthiopyridazine derivatives were synthesized and their hepatoprotective activities were screened in rat. The activities of these compounds were weaker than alkoxyallylthiopyridazine derivatives, which exhibit a superior hepatoprotective effect.

• Journal of the Korean Chemical Society
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• v.48 no.6
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• pp.609-615
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• 2004

Alkoxyallylthiopyridazine derivatives which exhibit superior effect for the treatment of hepatic diseases were synthesized from maleic anhydrides. The reaction of maleic anhydrides with hydrazine monohydrate in aq HCl at reflux afforded dihydroxypyridazines, which were transformed to dichloropyridazines with phosphorus oxychloride. The substitution of the first chlorine atom in dichloropyridazines proceeded selectively with alcoholic sodium alkoxides in THF to afford alkoxychloropyridazines, which were converted to alkoxyallylthiopyridazines with lithium 2-propene-1-thiolate in high yields.

• YAKHAK HOEJI
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• v.46 no.3
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• pp.155-160
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• 2002

Through a modification of allicin structure a disagreeable odor and chemical instability of allicin can be improved. 3-Alkoxy-6-allylthiopyridazine derivatives exhibit a superior effect for prevention and treatment of hepatic diseases induced by carbon tetrachloride and aflatoxin B1 and for prevention of human tissues from radiation. These compounds inhibit also efficiently SK-Hep-1 cell proliferation through induction of apoptosis. So another 4,5-mono- or di-substituted 3-alkyloxy-6-allylthiopyridazine derivatives were synthesized on purpose to find out SAR of allylthiopyridazine in hepatoprotective and hepatotherapeutic acitivitis and to develop more effective drug candidate.