title: Substituted piperidines--highly potent renin inhibitors due to induced fit adaptation of the active site.
abstract: The identification, synthesis and activity of a novel class of piperidine renin inhibitors is presented. The most active compounds show activities in the picomolar range and are among the most potent renin inhibitors ever identified.
authors.affiliation: Pharma Research Department, F. Hoffmann-La Roche Ltd, Basel, Switzerland.
authors.forename: E
authors.initials: E
authors.lastname: Vieira
authors.forename: A
authors.initials: A
authors.lastname: Binggeli
authors.forename: V
authors.initials: V
authors.lastname: Breu
authors.forename: D
authors.initials: D
authors.lastname: Bur
authors.forename: W
authors.initials: W
authors.lastname: Fischli
authors.forename: R
authors.initials: R
authors.lastname: Güller
authors.forename: G
authors.initials: G
authors.lastname: Hirth
authors.forename: H P
authors.initials: HP
authors.lastname: Märki
authors.forename: M
authors.initials: M
authors.lastname: Müller
authors.forename: C
authors.initials: C
authors.lastname: Oefner
authors.forename: M
authors.initials: M
authors.lastname: Scalone
authors.forename: H
authors.initials: H
authors.lastname: Stadler
authors.forename: M
authors.initials: M
authors.lastname: Wilhelm
authors.forename: W
authors.initials: W
authors.lastname: Wostl
mesh_terms: D001665:Binding Sites; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D010880:Piperidines / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors / Q000378:metabolism; D012083:Renin / Q000378:metabolism; D000092502:Renin Inhibitors
chemical_list: D010880:Piperidines; D011994:Recombinant Proteins; D012083:Renin; D000092502:Renin Inhibitors