title: 3,5-Diphenyl-1H-pyrazole derivatives. VI--Esters and 2-dialkylaminoethyl ethers of 1(2-hydroxy-2-phenylethyl)-3,5-diphenyl-1H-pyrazole and N,N-disubstituted 1-(2-amino-2-phenylethyl)-3,5-diphenyl-1H-pyrazoles with depressant and platelet antiaggregating activities.
abstract: The syntheses of 1-(2-hydroxy-2-phenylethyl)-3,5-diphenyl-1H-pyrazole 1 by reaction of 2-hydrazino-1-phenylethanol with dibenzoylmethane, of esters 2 and 2-dialkylaminoethyl ethers 3 starting from 1 as sodium salt and acyl chlorides or 2-chloroethyldialkylamines, respectively, as well as of N,N-disubstituted 1-(2-amino-2-phenylethyl)-3,5-diphenyl-1H-pyrazoles 5 by reaction of secondary amines with the tosylate of 1, 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.
authors.affiliation: Istituto di Scienze Farmaceutiche dell'Università Viale Benedetto XV, 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: C
authors.initials: C
authors.lastname: Losasso
authors.forename: L
authors.initials: L
authors.lastname: Stella
authors.forename: C
authors.initials: C
authors.lastname: de Paola
authors.forename: N
authors.initials: N
authors.lastname: Ioia
authors.forename: E
authors.initials: E
authors.lastname: Marmo
mesh_terms: 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
chemical_list: 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; C066207:1-(2-hydroxy-2-phenylethyl)-3,5-diphenylpyrazole