1. Cycloocta[b]pyran derivatives with local anesthetic, platelet antiaggregating and other activities.
- Author
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Longobardi M, Bargagna A, Mariani E, Schenone P, D'Amico M, Falciani M, Filippelli W, and Contaldi C
- Subjects
- Anesthetics, Local pharmacology, Animals, Anti-Arrhythmia Agents pharmacology, Anti-Inflammatory Agents, Non-Steroidal pharmacology, Humans, Mice, Platelet Aggregation Inhibitors pharmacology, Pyrans pharmacology, Rats, Anesthetics, Local chemical synthesis, Anti-Arrhythmia Agents chemical synthesis, Anti-Inflammatory Agents, Non-Steroidal chemical synthesis, Platelet Aggregation Inhibitors chemical synthesis, Pyrans chemical synthesis
- Abstract
The synthesis of some N,N-disubstituted 4-amino-5,6,7,8,9,10-hexahydro-3- phenyl-2H-cycloocta[b]pyran-2-ones by reaction of phenylchloroketene with a series of N,N-disubstituted 2-aminomethylenecyclooctanones, followed by dehydrochlorination in situ of the primary adducts with DBN, is described. The dimethylamino derivative showed a local anesthetic activity in mice superior to that of lidocaine, and some compounds exhibited a platelet antiaggregating activity in vitro superior or comparable to that of acetylsalicylic acid, as well as weak antiarrhythmic and antiinflammatory activities in rats. more...
- Published
- 1995