Synthesis and pharmacological evaluation of 2,5-cycloamino-5H-[1]benzopyrano[4,3-d]pyrimidines endowed with in vitro antiplatelet activity

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'-dip...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2001-06, Vol.11 (11), p.1397-1400
Main Authors: BRUNO, O, BRULLO, C, RANISE, A, SCHENONE, S, BONDAVALLI, F, BAROCELLI, E, BALLABENI, V, CHIAVARINI, M, TOGNOLINI, M, IMPICCIATORE, M
Format: Article
Language:English
Subjects:
Adenosine Diphosphate - metabolism
Analgesics - chemical synthesis
Analgesics - chemistry
Analgesics - pharmacology
Analgesics - therapeutic use
Animals
Anti-Inflammatory Agents - chemical synthesis
Anti-Inflammatory Agents - chemistry
Anti-Inflammatory Agents - pharmacology
Anti-Inflammatory Agents - therapeutic use
Arachidonic Acid - metabolism
Benzopyrans - chemical synthesis
Benzopyrans - chemistry
Benzopyrans - pharmacology
Benzopyrans - therapeutic use
Biological and medical sciences
Blood. Blood coagulation. Reticuloendothelial system
Collagen - metabolism
Disease Models, Animal
Edema - drug therapy
Guinea Pigs
Medical sciences
Pain - drug therapy
Pharmacology. Drug treatments
Platelet Aggregation - drug effects
Platelet Aggregation Inhibitors - chemical synthesis
Platelet Aggregation Inhibitors - chemistry
Platelet Aggregation Inhibitors - pharmacology
Platelet Aggregation Inhibitors - therapeutic use
Pyrimidines - chemical synthesis
Pyrimidines - chemistry
Pyrimidines - pharmacology
Pyrimidines - therapeutic use
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Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(01)00221-9