title: Drug discovery: phosphinolactone, in vivo bioisostere of the lactol group.
abstract: In drug discovery, structural modifications over the lead molecule are often crucial for the development of a drug. Herein, we reported the first in vivo bioisosteric effect of phosphinolactone function in relation to the lactol group constituting the bioactive molecule: Hydroxybupropion. The preparation of phosphinolactone analogues and their antidepressant evaluation towards forced swimming test in mice showed that biological activity was regained and even strengthen.
authors.affiliation: Institut Charles Gerhardt Montpellier, ENSCM, 8 rue de l'Ecole Normale, 34296, Montpellier Cedex 5, France. jean-noel.volle@enscm.fr
authors.forename: Jean-Noël
authors.initials: JN
authors.lastname: Volle
authors.forename: Damien
authors.initials: D
authors.lastname: Filippini
authors.forename: Bartlomiej
authors.initials: B
authors.lastname: Krawczy
authors.forename: Nikolay
authors.initials: N
authors.lastname: Kaloyanov
authors.forename: Arie
authors.initials: A
authors.lastname: Van der Lee
authors.forename: Tangui
authors.initials: T
authors.lastname: Maurice
authors.forename: Jean-Luc
authors.initials: JL
authors.lastname: Pirat
authors.forename: David
authors.initials: D
authors.lastname: Virieux
mesh_terms: D000818:Animals; D000928:Antidepressive Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001522:Behavior, Animal / Q000187:drug effects; D055808:Drug Discovery; D007783:Lactones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D008297:Male; D051379:Mice; D008958:Models, Molecular; D008968:Molecular Conformation; D010721:Phosphinic Acids / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013237:Stereoisomerism; D013550:Swimming
chemical_list: D000928:Antidepressive Agents; D007783:Lactones; D010721:Phosphinic Acids