title: Phosphodiesterase inhibitory properties of losartan. Design and synthesis of new lead compounds.
abstract: A 4-centre PDE4 pharmacophore search has been carried out in several 3D-databases containing compounds belonging to different therapeutic areas. Losartan, an angiotensin-II antagonist, has been identified as a new lead compound for developing PDE4 inhibitors. New families of compounds derived from losartan has been synthesized and their PDE inhibition has been measured.
authors.affiliation: Almirall Prodesfarma Research Center, Barcelona, Spain.
authors.forename: V
authors.initials: V
authors.lastname: Segarra
authors.forename: M I
authors.initials: MI
authors.lastname: Crespo
authors.forename: F
authors.initials: F
authors.lastname: Pujol
authors.forename: J
authors.initials: J
authors.lastname: Beleta
authors.forename: T
authors.initials: T
authors.lastname: Doménech
authors.forename: M
authors.initials: M
authors.lastname: Miralpeix
authors.forename: J M
authors.initials: JM
authors.lastname: Palacios
authors.forename: A
authors.initials: A
authors.lastname: Castro
authors.forename: A
authors.initials: A
authors.lastname: Martinez
mesh_terms: D000818:Animals; D015195:Drug Design; D006168:Guinea Pigs; D006352:Heart Ventricles / Q000187:drug effects / Q000201:enzymology; D066298:In Vitro Techniques; D019808:Losartan / Q000737:chemistry / Q000494:pharmacology*; D010726:Phosphodiesterase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D010726:Phosphodiesterase Inhibitors; D019808:Losartan