Amidino-Containing Schiff Base Copper(II) and Iron(III) Chelates as a Thrombin Inhibitor
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- Toyota Eiko
- Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido
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- Sekizaki Haruo
- Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido
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- Takahashi Yu-u
- Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido
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- Itoh Kunihiko
- Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido
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- Tanizawa Kazutaka
- Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido
書誌事項
- タイトル別名
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- Amidino Containing Schiff Base Copper 2 and Iron 3 Chelates as a Thrombin Inhibitor
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抄録
Four series of Schiff base copper(II) and iron(III) chelates were synthesized from 4-formyl-3-hydroxybenzamidine or 3-formyl-4-hydroxybenzamidine and various L- or D-amino acids. Their inhibitory activities for bovine α-thrombin (abbreviated as thrombin) were determined. The most potent thrombin inhibitor in this series is copper(II) chelate (1g′) derived from 4-formyl-3-hydroxybenzamidine and D-Trp. Its Ki value, 2.7×10−8 M, is comparable to that of Argatroban (MD-805), which is a clinically used compound. The iron(III) chelates derived from 4-formyl-3-hydroxybenzamidine and hydrophobic L-amino acids (Val, Ile, Leu, Phe, Trp, Met) also exhibited higher inhibitory potency. It appears that coordination geometry composed of metal ion, amidino group, amino acid side chain is well accommodated to the thrombin active site. From the Ki values of Schiff base metal chelates for thrombin, the structure–activity relationships between the chelates and active site of thrombin were discussed.
収録刊行物
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- CHEMICAL & PHARMACEUTICAL BULLETIN
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CHEMICAL & PHARMACEUTICAL BULLETIN 53 (1), 22-26, 2005
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390001204170868480
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- NII論文ID
- 10016651296
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- NII書誌ID
- AA00602100
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- ISSN
- 13475223
- 00092363
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- NDL書誌ID
- 7200655
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- PubMed
- 15635223
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可