Abstract
Pyrrolo-benzylisoquinolines were prepared as target compounds and their antiplatelet aggregation activity, adreno-receptor affinity, and cytotoxicity were screened. Compounds 1d-9d showed specific antiplatelet aggregation activity induced by arachidonic acid and collagen. Among them, 8d and 9d exhibited better activity than the reference drug, aspirin and 9d also showed inhibition of platelet aggregation by all four inducers.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adrenergic Antagonists / metabolism
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Adrenergic Antagonists / pharmacology
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Animals
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Arachidonic Acid / antagonists & inhibitors
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Aspirin / pharmacology
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Benzyl Compounds / chemistry
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Benzyl Compounds / metabolism
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Benzyl Compounds / pharmacology
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Collagen / antagonists & inhibitors
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Guinea Pigs
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Humans
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Inhibitory Concentration 50
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Isoquinolines / chemistry*
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Isoquinolines / metabolism
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Isoquinolines / pharmacology*
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Platelet Aggregation / drug effects
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Platelet Aggregation Inhibitors / pharmacology*
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Propanolamines / metabolism
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Propanolamines / pharmacology
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Pyrroles / chemistry*
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Pyrroles / metabolism
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Pyrroles / pharmacology*
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Structure-Activity Relationship
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Tumor Cells, Cultured
Substances
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Adrenergic Antagonists
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Benzyl Compounds
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Isoquinolines
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Platelet Aggregation Inhibitors
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Propanolamines
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Pyrroles
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Arachidonic Acid
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Collagen
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Aspirin
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CGP 12177