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-50-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.
Synthesis and pharmacological evaluation of 2,5-Cycloamino-5H[1]benzopyrano[4,3-d]pyrimidines endowed with in vitro antiplatelet activity
BRUNO, OLGA;BRULLO, CHIARA;RANISE, ANGELO;SCHENONE, SILVIA;BONDAVALLI, FRANCESCO;
2001
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-50-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.
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