Abstract
A series of new 2,5-cycloamino-5H-[1]benzopyrano[4,3-d]pyrimidines 3a-i have been synthesized and tested in vivo for the anti-inflammatory/analgesic/antipyretic effects and in vitro to evaluate the antiplatelet activity on guinea-pig platelet-rich plasma aggregated by collagen, adenosine-5'-diphosphate (ADP) and arachidonic acid (AA). Title compounds were ineffective in vivo; however, the pyrrolidino derivatives 3a and 3c exhibited an antiplatelet activity against all the aggregants differing from that of acetylsalicylic acid (ASA) while the 5-morpholino derivatives 3g-i showed the most potent ASA-like antiplatelet activity.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adenosine Diphosphate / metabolism
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Analgesics / chemical synthesis
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Analgesics / chemistry
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Analgesics / pharmacology
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Analgesics / therapeutic use
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Animals
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Anti-Inflammatory Agents / chemical synthesis
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Anti-Inflammatory Agents / chemistry
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Anti-Inflammatory Agents / pharmacology
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Anti-Inflammatory Agents / therapeutic use
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Arachidonic Acid / metabolism
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Benzopyrans / chemical synthesis*
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Benzopyrans / chemistry
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Benzopyrans / pharmacology
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Benzopyrans / therapeutic use
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Collagen / metabolism
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Disease Models, Animal
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Edema / drug therapy
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Guinea Pigs
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Pain / drug therapy
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Platelet Aggregation / drug effects
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Platelet Aggregation Inhibitors / chemical synthesis*
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Platelet Aggregation Inhibitors / chemistry
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Platelet Aggregation Inhibitors / pharmacology
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Platelet Aggregation Inhibitors / therapeutic use
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Pyrimidines / chemical synthesis*
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Pyrimidines / chemistry
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Pyrimidines / pharmacology
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Pyrimidines / therapeutic use
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Rats
Substances
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Analgesics
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Anti-Inflammatory Agents
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Benzopyrans
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Platelet Aggregation Inhibitors
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Pyrimidines
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Arachidonic Acid
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Adenosine Diphosphate
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Collagen