2-Amino-Benzo[d]isothiazol-3-one derivatives: synthesis and assessment of their antiplatelet/spasmolytic effects.
We describe a series of 2-amino-benzo[d]isothiazol-3-one derivatives (2-8), which were synthesized and screened in vitro for inhibition of platelet aggregation and for their spasmolytic activity, with the awareness that the development of antiplatelet agents with additional vasodilation activity could be beneficial in the treatment of various vaso-occlusive disorders. The tested compounds show a powerful antiplatelet activity and various modifications resulted in molecules possessing antiaggregating effects as well as spasmolytic actions.
Vicini
P
P
Dipartimento Farmaceutico, Università degli Studi Parma, Italy. pvicini@ipruniv.cce.unipr.it
Amoretti
L
L
Ballabeni
V
V
Tognolini
M
M
Barocelli
E
E
D000244:Adenosine Diphosphate / Q000494:pharmacology; D000818:Animals; D001011:Aorta / Q000187:drug effects; D016718:Arachidonic Acid / Q000494:pharmacology; D001547:Benzaldehydes / Q000138:chemical synthesis / Q000494:pharmacology; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D020128:Inhibitory Concentration 50; D008297:Male; D023421:Models, Animal; D009119:Muscle Contraction / Q000187:drug effects; D010276:Parasympatholytics / Q000138:chemical synthesis* / Q000494:pharmacology; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D013844:Thiazoles / Q000138:chemical synthesis / Q000494:pharmacology*
D001547:Benzaldehydes; D010276:Parasympatholytics; D010975:Platelet Aggregation Inhibitors; D013844:Thiazoles; D016718:Arachidonic Acid; D000244:Adenosine Diphosphate