Abstract
The syntheses of 1-(2-hydroxy-3-phenoxypropyl)-3,5-diphenyl-1H-pyrazole 2 by reaction of 1-hydrazino-3-phenoxy-2-propranolol with dibenzoylmethane, of esters 3 and 2-dialkylaminoethyl ethers 4 starting from 2 as sodium salt and acyl chlorides or 2-chloroethyldialkylamines, respectively, as well as of N-aryl carbamates 5 by reaction of 2 with aryl isocyanates, are described. Some of the above compounds showed a considerable sedative effect in mice and a remarkable platelet antiaggregating activity in vitro, as well as moderate local anesthetic, analgesic and antiinflammatory activities in mice and rats.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Anesthetics, Local / chemical synthesis
-
Animals
-
Anti-Arrhythmia Agents / chemical synthesis
-
Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis
-
Antihypertensive Agents / chemical synthesis
-
Central Nervous System Depressants / chemical synthesis*
-
Chemical Phenomena
-
Chemistry
-
Humans
-
In Vitro Techniques
-
Mice
-
Motor Activity / drug effects
-
Platelet Aggregation / drug effects*
-
Platelet Aggregation Inhibitors / chemical synthesis*
-
Pyrazoles / chemical synthesis*
-
Pyrazoles / pharmacology
-
Rats
Substances
-
Anesthetics, Local
-
Anti-Arrhythmia Agents
-
Anti-Inflammatory Agents, Non-Steroidal
-
Antihypertensive Agents
-
Central Nervous System Depressants
-
Platelet Aggregation Inhibitors
-
Pyrazoles