Substituted piperidines--highly potent renin inhibitors due to induced fit adaptation of the active site.
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.
Vieira
E
E
Pharma Research Department, F. Hoffmann-La Roche Ltd, Basel, Switzerland.
Binggeli
A
A
Breu
V
V
Bur
D
D
Fischli
W
W
Güller
R
R
Hirth
G
G
Märki
H P
HP
Müller
M
M
Oefner
C
C
Scalone
M
M
Stadler
H
H
Wilhelm
M
M
Wostl
W
W
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
D010880:Piperidines; D011994:Recombinant Proteins; D012083:Renin; D000092502:Renin Inhibitors