新規カルシウム拮抗薬(+)-(R)-3,4-Dihydro-2-[5-methoxy-2-[3-[N-methyl-N-[2-[(3,4-methylenedioxy)phenoxy]ethyl]aminol]propoxy]phenyl]-4-methyl-3-oxo-2H-1,4-benzothiazine(SD-3211)のラット糞中代謝物の合成とそのカルシウム拮抗作用

概要

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In order to confirm the structure of three fecal metabolites, M-I, M-II and M-III, of a new calcium antagonist, (+)-3,4-dihydro-2-[5-methoxy-2-[3-[N-methyl-N-[2-[(3,4-methylenedioxy) phenoxyl] ethyl] amino] propoxy] phenyl]-4-methyl-3-oxo-2H-1,4-benzothiazine (SD-3211), in rats, (+)-3,4-dihydro-2-[5-hydroxy-2-[3-[N-methyl-N-[2-[(3,4-methylenedioxy)-phenoxy] ethyl] amino] propoxy] phenyl]-4-methyl-3-oxo-2H-1,4-benzothiazine ((+)-I), (+)-3,4-dihydro-2-[5-hydroxy-2-[3-[N-[2-[(3,4-methylenedioxy) phenoxy] ethyl] amino] propoxy]-phenyl]-4-methyl-3-oxo-2H-1,4-benzothiazine ((+)-II) and (+)-3,4-dihydro-2-[5-methoxy-2-[3-[N-[2-[(3,4-methylenedioxy) phenoxy] ethyl] amino] propoxy] phenyl]-4-methyl-3-oxo-2H-1,4-benzothiazine ((+)-III) were synthesized. Compounds (+)-I, (+)-II and (+)-III were identified with the fecal metabolites M-I, M-II and M-III, respectively. The calcium antagonistic activities of (+)-I, (+)-II and (+)-III were examined.
公益社団法人日本薬学会の論文
1991-01-25