3,5-Diphenyl-1H-pyrazole derivatives. VII--Esters, 2-dialkylaminoethyl ethers and N-substituted carbamates of 1-(2-hydroxy-3-phenoxypropyl)-3,5-diphenyl-1H-pyrazole with depressant and platelet antiaggregating activities.
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.
Bruno
O
O
Istituto di Scienze Farmaceutiche dell'Università Viale Benedetto XV, Genova, Italy.
Bondavalli
F
F
Ranise
A
A
Schenone
P
P
Losasso
C
C
Cenicola
M L
ML
Stella
L
L
Donnoli
D
D
Marmo
E
E
D000779:Anesthetics, Local / Q000138:chemical synthesis; D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000138:chemical synthesis; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis; D000959:Antihypertensive Agents / Q000138:chemical synthesis; D002492:Central Nervous System Depressants / Q000138:chemical synthesis*; D055598:Chemical Phenomena; D002621:Chemistry; D006801:Humans; D066298:In Vitro Techniques; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis*; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats
D000779:Anesthetics, Local; D000889:Anti-Arrhythmia Agents; D000894:Anti-Inflammatory Agents, Non-Steroidal; D000959:Antihypertensive Agents; D002492:Central Nervous System Depressants; D010975:Platelet Aggregation Inhibitors; D011720:Pyrazoles