One-step synthesis and pharmacological activity of new (N-substituted)amino-spiroalkan-dione derivatives.
The synthesis of (N-substituted)amino-spiroalkan-dione derivatives 3 is described starting from enamines 1 and carbon suboxide 2, and their inhibitory effects on blood coagulation in vivo and on platelet aggregation in vitro are determined. Some of synthesized compounds showed a strong anticoagulant activity. A comparative pharmacological study of the anticoagulant effects of the new compounds versus Warfarin suggests that their behaviour is analogous, though the action mechanism is different.
Bonsignore
L
L
Dipartimento Farmaco Chimico Tecnologico, Università di Cagliari, Italy.
Loy
G
G
Cottiglia
F
F
Calignano
A
A
D000244:Adenosine Diphosphate / Q000494:pharmacology; D000818:Animals; D003094:Collagen / Q000494:pharmacology; D003503:Cyclobutanes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D010972:Platelet Activating Factor / Q000494:pharmacology; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D012015:Reference Standards; D013057:Spectrum Analysis; D013141:Spiro Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D003503:Cyclobutanes; D010972:Platelet Activating Factor; D010975:Platelet Aggregation Inhibitors; D013141:Spiro Compounds; D000244:Adenosine Diphosphate; D003094:Collagen