title: 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.
abstract: 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.
authors.affiliation: Istituto di Scienze Farmaceutiche, Università di Genova, Italy.
authors.forename: F
authors.initials: F
authors.lastname: Bondavalli
authors.forename: O
authors.initials: O
authors.lastname: Bruno
authors.forename: A
authors.initials: A
authors.lastname: Ranise
authors.forename: P
authors.initials: P
authors.lastname: Schenone
authors.forename: S
authors.initials: S
authors.lastname: Russo
authors.forename: A
authors.initials: A
authors.lastname: Loffreda
authors.forename: V
authors.initials: V
authors.lastname: De Novellis
authors.forename: C
authors.initials: C
authors.lastname: Lo Sasso
authors.forename: E
authors.initials: E
authors.lastname: Marmo
mesh_terms: 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
chemical_list: D000700:Analgesics; D000779:Anesthetics, Local; D000889:Anti-Arrhythmia Agents; D000894:Anti-Inflammatory Agents, Non-Steroidal; D011720:Pyrazoles; D008315:Malondialdehyde; D001966:Bromine