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박명숙(Myung Sook Park),윤명선(Myung Sun Yun),김미경(Mi Kyung Kim),권순경(Soon Kyung Kwon) 대한약학회 2001 약학회지 Vol.45 No.6
In order to discover new useful NSAIDS, novel N-substituted 1,2-benzisothiazoline-3- one 1,1-dioxide derivatives, which can exhibit potentially antiinflammatory activity were synthesized.1,2-Benzisothiazoline-3-one-N-acetic acids 6a, b were obtained from monochloroacetic acid and sodium 1,2-benzisothiazoline-3-ones in DMF by N- al1kylation reaction. N-Substituted 1,2-benzisothiazoline-3-one 1,1-dioxice derivatives 7a-e were synthesized through the coupling of compound 6a, b and several amines (aniline, 2-aminopyridine, 2- aminothiazole, 2-aminotetrazole) with dicyclohexylcarbodiimide in methylene chloride.
Benzo(a)pyrene의 돌연변이원성에 대한 유기게르마늄(GE-132)의 항돌연변이 효과
이효민(Hyo Min Lee),정용(Yong Chung),정기화(Ki Why Jung),김재완(Jae Wan Kim),권순경(Sun Kyung Kwon) 대한약학회 1993 약학회지 Vol.37 No.1
This study was initiated to investigate the effective action and mechanism of GE-132 (Carboxyethylgermanium sesquioxide)on benzo(a)pyrene, which have strong carcinogenicity and mutagenicity. To confirm desmutagenic effect (inhibition of metabolic processes of benzo(a)pyrene with S9 Mix or inactivation of the mutagenicity of benzo(a)pyrene metabolites) and antimutagenic effect (inhibition of gene-expression of reverted genes) of GE-132 against benzo(a)pyrene using with Salmonella typhimurium TA98 Ames test was performed. The revertants in desmutagenicity test were decreased significantly in the combined groups of benzo(a)pyrene and GE-132 than benzo(a)pyrene only, without inhibition the metabolism of benzo(a)pyrene by S9 Mix. The ideal combined groups of benzo(a)pyrene and GE-132 were lOmcM and 10mg, 20mcM and 20mg, lOOmcM and 30mg, respectively. Then, the revertants in antimutagenicity test, which was studied the direct action of GE-132 on the induction of revertant cells by Salmonella typhimurium TA98 and activated benzo(a)pyrene were decreased significantly in the treated groups of GE-132 than no treated groups. The number of revertants of Salmonella typhimurium TA98 were reduced with increasing amounts of GE-132. From the above results, it was found that GE-132 inactivated the mutagenic metabolites of benzo(a)pyrene without inhibition of the enzyme action in the S9 Mix, and GE-132 showed antimutagenic effect which have inhibitory action of reverted gene expression.