3,5-Diphenyl-1H-pyrazole derivatives. V--1-Acetyl-4-hydroxy-3,5-diphenyl-2-pyrazoline esters, 4-hydroxy-3,5-diphenyl-1H-pyrazole esters and N-substituted 4-(3-amino-2-hydroxy-1-propoxy)-1-methyl-3,5-diphenyl-1H-pyrazoles with antiarrhythmic, sedative and platelet antiaggregating activities.
The synthesis of 1-acetyl-4-hydroxy-3,5-diphenyl-2-pyrazoline esters 3, 4-hydroxy-3,5-diphenyl-1H-pyrazole esters 5 and N-substituted 4-(3-amino-2-hydroxy-1-propoxy)-1-methyl-3,5-diphenyl-1H-pyrazoles 7, starting from 4-hydroxy-3,5-diphenyl-2-pyrazoline is described. Some of compounds 3, 5 and 7 showed a considerable antiarrhythmic and sedative activity in rats and mice, respectively, as well as a remarkable in vitro platelet antiaggregating activity. Moreover, the above compounds usually exhibited moderate antihypertensive, local anesthetic, analgesic and antiinflammatory activities in rats and mice.
Bruno
O
O
Istituto di Scienze Farmaceutiche dell'Università, Genova, Italy.
Bondavalli
F
F
Ranise
A
A
Schenone
P
P
Losasso
C
C
Cilenti
L
L
Matera
C
C
Marmo
E
E
D000700:Analgesics / Q000138:chemical synthesis / Q000494:pharmacology; D000779:Anesthetics, Local / Q000138:chemical synthesis / Q000494:pharmacology; D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000138:chemical synthesis*; D000959:Antihypertensive Agents / Q000138:chemical synthesis / Q000494:pharmacology; D004952:Esters / Q000138:chemical synthesis / Q000494:pharmacology; D006801:Humans; D006993:Hypnotics and Sedatives / Q000138:chemical synthesis*; D066298:In Vitro Techniques; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis*; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats
D000700:Analgesics; D000779:Anesthetics, Local; D000889:Anti-Arrhythmia Agents; D000959:Antihypertensive Agents; D004952:Esters; D006993:Hypnotics and Sedatives; D010975:Platelet Aggregation Inhibitors; D011720:Pyrazoles