3,5-Diphenyl-1H-pyrazole derivatives. II--N-substituted 1-(2-aminoethyl)-3,5-diphenyl-1H-pyrazoles and their 4-bromo derivatives with analgesic and other activities.
The synthesis of N-substituted 1-(2-aminoethyl)-3,5-diphenyl-1H-pyrazoles and their 4-bromo derivatives (V) by reaction of primary and secondary amines with the tosylates of 1-(2-hydroxyethyl)-3,5-diphenyl-1H-pyrazole and its 4-bromo derivative is described. Some of compounds (V) showed a remarkable analgesic activity in mice. Moreover, the above compounds usually exhibited moderate hypotensive, bradycardiac and antiinflammatory activities in rats, infiltration anesthesia in mice, as well as a weak platelet antiaggregating activity in vitro.
Bondavalli
F
F
Istituto di Scienze Farmaceutiche, Università di Genova, Italy.
Bruno
O
O
Ranise
A
A
Schenone
P
P
Russo
S
S
Loffreda
A
A
De Novellis
V
V
Lo Sasso
C
C
Marmo
E
E
D000700:Analgesics / Q000138:chemical synthesis*; D000779:Anesthetics, Local; D000818:Animals; D000889:Anti-Arrhythmia Agents; D000894:Anti-Inflammatory Agents, Non-Steroidal; D001792:Blood Platelets / Q000187:drug effects / Q000378:metabolism; D001794:Blood Pressure / Q000187:drug effects; D001966:Bromine / Q000138:chemical synthesis / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D006339:Heart Rate / Q000187:drug effects; D008315:Malondialdehyde / Q000097:blood; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats
D000700:Analgesics; D000779:Anesthetics, Local; D000889:Anti-Arrhythmia Agents; D000894:Anti-Inflammatory Agents, Non-Steroidal; D011720:Pyrazoles; D008315:Malondialdehyde; D001966:Bromine