Synthesis and Pharmacological Activity of the Metabolites of Pratosartan
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概要
- 論文の詳細を見る
Three hydroxylated metabolites of 2-propyl-3-[2'-(1H-tetrazol-5-yl)biphenyl-4-ylmethyl]-5,6,7,8-tetrahydro-3H-cycloheptimidazol-4-one (Pratosartan), which is a selective angiotensin II receptor antagonist, were synthesized in confirmation of their structures and in studies of their pharmacological properties. An MTPA ester of the human main metabolite was identified with the synthesized compound by comparing ^1H-NMR spectra, MS spectra, and HPLC retention time. The structure of the human main metabolite was confirmed to be (S)-(-)-2-(1-hydroxypropyl)-3-[2'-(1H-tetrazol-5-yl)biphenyl-4-ylmethyl]-5,6,7,8-tetrahydro-3H-cycloheptimidazol-4-one ((S)-(-)-1). Also, the rat main metabolites were confirmed to be 8-hydroxylated compound (2) and 5-hydroxylated compound (3). These metabolites showed lower antagonistic activity than that of the parent compound.
- 公益社団法人日本薬学会の論文
- 2006-06-01
著者
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Tomiyama Akira
Kotobuki Research Laboratories Kotobuki Seiyaku Company Ltd.
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Sonegawa Motoharu
Kotobuki Research Laboratories Kotobuki Seiyaku Company Ltd.
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Tomiyama Tsuyoshi
Kotobuki Research Laboratories Kotobuki Seiyaku Company Ltd.
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SUZAKA Hiroaki
Kotobuki Research Laboratories, Kotobuki Seiyaku Company, Ltd.
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Suzaka Hiroaki
Kotobuki Research Laboratories Kotobuki Seiyaku Company Ltd.
関連論文
- Change of Mechanical Activity to Contraction from the Relaxation Induced by the Intracellular Ca^ Antagonist KT-362; Effects of Alkylation of Side Chain, and Substitution of 2,3,4,5-Tetrahydro-1,5-Benzothiazepine Derivatives
- Synthesis and Pharmacological Activity of the Metabolites of Pratosartan
- Regioselective Alkylation of 2-Alkyl-5,6,7,8-tetrahydro-3H-cycloheptimidazol-4-ones and 2-Alkyl-3H-cycloheptimidazol-4-ones
- Effective Preparation of Cycloheptimidazol-4-one Compounds