Thromboxane A2 receptor antagonists. I. Synthesis and pharmacological activity of 7-oxabicyclo-(2.2.1)heptane derivatives with the benzenesulfonylamino group.
書誌事項
- 公開日
- 1989
- 資源種別
- journal article
- DOI
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- 10.1248/cpb.37.327
- 公開者
- 公益社団法人 日本薬学会
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説明
Four stereoisomers of 7-oxabicyclo[2.2.1]heptane derivatives with the benzenesulfonylamino group, 11, 14, 23 and 33, were synthesized and their sodium salts were examined in vitro for inhibitory activity against aggregation of rabbit platelet-ric plasma and of rat washed platelets. The trans-isomer 23 exhibited high potency but showed a partial agonistic effect. Compound 11 did not show a partial agonistic effect, though it was a less active inhibitor. The following trans compounds were synthesized and their IC50 values were measured : homologated trans-isomers with one methylene chain (47 and 53), an olefin derivative (58), and optically active derivatives ((-)-11 and (+)-23).
収録刊行物
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- ＣＨＥＭＩＣＡＬ ＆ ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ ＢＵＬＬＥＴＩＮ
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ＣＨＥＭＩＣＡＬ ＆ ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ ＢＵＬＬＥＴＩＮ 37 (2), 327-335, 1989
公益社団法人 日本薬学会