Thromboxane A_2 Receptor Antagonists. I. : Synthesis and Pharmacological Activity of 7-Oxabicyclo-[2.2.1]heptane Derivatives with the Benzenesulfonylamino Group

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概要

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• 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 IC_<50> values were measured : homologated trans-isomers with one methylene chain (47 and 53), an olefin derivative (58), and optically active derivatives ((-)-11 and (+)-23).

• 公益社団法人日本薬学会の論文
• 1989-02-25

著者

• 萩下 山治

  Shionogi Research Laboratories Shionogi & Co. Ltd.

• 瀬野 薫

  Shionogi Research Laboratories, Shinogi & Co., Ltd.,

• 瀬野 薫

  Shionogi Research Laboratories Shionogi & Co. Ltd.

関連論文

• A Novel Class of Platelet Activating Factor (PAF) Antagonists. II. Modification of the 2-Position of the Glycerol Backbone of PAF-Sulfonamide Isosteres
• Synthesis and Absolute Configuration of (+)-threo-1-Hydroxy-2-(isopropylamino)-[10]-paracyclophane
• Thromboxane A_2 Receptor Antagonists. III. : Synthesis and Pharmacological Activity of 6,6-Dimethylbicyclo[3.1.1]heptane Derivatives with a Substituted Sulfonylamino Group at C-2
• Thromboxane A_2 Receptor Antagonists. II. : Synthesis and Pharmacological Activity of 6,6-Dimethylbicyclo[3.1.1]heptane Derivatives with the Benzenesulfonylamino Group
• Thromboxane A_2 Receptor Antagonists. I. : Synthesis and Pharmacological Activity of 7-Oxabicyclo-[2.2.1]heptane Derivatives with the Benzenesulfonylamino Group

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