title: Synthesis and pharmacological screening of new phenylpiperazinepropane derivatives and their enantiomers.
abstract: Enantiomers of phenylpiperazinepropane-1,2-diol derivatives were synthesized with the purpose to obtain a better antitussive activity/sedative effect ratio. (S)-isomers showed better pharmacological profiles than (R)-isomers and corresponding racemates. Among the (S)-isomers, the unsubstituted compound, levodropropizine (S(-)-3-(4-phenyl-piperazin-1-yl)-propane-1,2-diol, DF 526), has the most favourable antitussive activity/sedative effect ratio and was selected for pharmaco-toxicological evaluation.
authors.affiliation: Research & Development Laboratories, Dompé Farmaceutici S.p.A., Milan, Italy.
authors.forename: R
authors.initials: R
authors.lastname: Giani
authors.forename: E
authors.initials: E
authors.lastname: Marinone
authors.forename: G
authors.initials: G
authors.lastname: Melillo
authors.forename: M
authors.initials: M
authors.lastname: Borsa
authors.forename: G C
authors.initials: GC
authors.lastname: Tonon
mesh_terms: D000818:Animals; D000996:Antitussive Agents / Q000009:adverse effects / Q000138:chemical synthesis*; D055598:Chemical Phenomena; D002621:Chemistry; D006168:Guinea Pigs; D007536:Isomerism; D008297:Male; D051379:Mice; D011409:Propylene Glycols / Q000009:adverse effects / Q000138:chemical synthesis*; D012890:Sleep / Q000187:drug effects
chemical_list: D000996:Antitussive Agents; D011409:Propylene Glycols; C035916:dipropizine