Synthesis and Evaluation of Coumarin α-Methylene-γ-butyrolactones : A New Class of Platelet Aggregation Inhibitors

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概要

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• In a search for new inhibitors of platelet aggregation, certain coumarin-bearing α-methylene-γ-butyrolactones were synthesized and evaluated for inhibitory activity against thrombin (Thr)-, arachidonic acid (AA)-, collagen (Col)-, and platelet-activating factor (PAF)-induced aggregation in washed rabbit platelets. These compounds were efficiently synthesized from commercially available 7-hydroxycoumarin or its derivative. Among them, 7-[(2,3,4,5-tetrahydro-4-methylene-5-oxo-2-phenyl-2-furanyl)methoxy]-2H-1-benzopyran-2-one (3d) showed the most potent inhibition of AA- and PAF- induced aggregation, with IC_<50> values of 3.65 and 16.36μM respectively.

• 公益社団法人日本薬学会の論文
• 1996-08-15

著者

• Tzeng C‐c

  Kaohsiung Medical Univ. Kaohsiung City Twn

• Teng C‐m

  National Taiwan Univ. Taipei Twn

• Teng Che-ming

  Pharmacological Institute College Of Medicine National Taiwan University

• CHEN Yeh-Long

  School of Chemistry, Kaohsiung Medical College

• WANG Tai-Chi

  School of Chemistry, Kaohsiung Medical College

• LIANG Shiu-Chuan

  Pharmacological Institute, College of Medicine, National Taiwan University

• TZENG Cherng-Chyi

  School of Chemistry, Kaohsiung Medical College

• Chen Y‐l

  Kaohsiung Medical Coll. Kaohsiung Twn

• Chang Ya-ling

  School Of Chemistry Kaohsiung Medical College:department Of Chemistry National Sun Yat-sen Universit

• Wang T‐c

  Tajen Inst. Of Technol. Pintung Twn

• Liang Shiu-chuan

  Pharmacological Institute College Of Medicine National Taiwan University

• Tzeng Cherng-chyi

  School Of Chemistry Kaohsiung Medical University

関連論文

• Synthesis and Antiplatelet, Antiinflammatory and Antiallergic Activities of 2,3-Disubstituted 1,4-Naphthoquinones
• Synthesis of 2-Alkoxy 1,4-Naphthoquinone Derivatives as Antiplatelet, Antiinflammatory, and Antiallergic Agents
• Synthesis and Evaluation of Coumarin α-Methylene-γ-butyrolactones : A New Class of Platelet Aggregation Inhibitors
• Antiplatelet Effect and Selective Binding to Cyclooxygenase by Molecular Docking Analysis of 3-Alkylaminopropoxy-9,10-anthraquinone Derivatives(Medicinal Chemistry)
• α-Methylene-γ-butyrolactones : Synthesis and Vasorelaxing Activity Assay of Coumarin, Naphthalene, and Quinoline Derivatives
• Synthesis and Antiplatelet Evaluation of α-Methylene-γ-butyrolactone Bearing 2-Methylquinoline and 8-Hydroxyquinoline Moieties
• Synthesis and Anti-platelet, Anti-inflammatory and Anti-allergic Activities of Methoxyisoflavanquinone and Related Compounds
• Effect of PP1D-1, a Synthetic Antiplatelet Compound, on Rabbit Platelets
• The Inhibitory Mechanism of YC-1, a Benzyl Indazole, on Smooth Muscle Cell Proliferation : an In Vitro and In Vivo Study
• Crystal Structure of 3-Amino-1,2,4-triazin-5(2H)-one
• Ca2+-Channel Blockade in Rat Thoracic Aorta by Protopine Isolated from Corydalis Tubers.

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