New classes of potent and bioavailable human renin inhibitors.
New classes of de novo designed renin inhibitors are reported. Some of these compounds display excellent in vitro and in vivo activities toward human renin in a TGR model. The synthesis of these new types of mono- and bicyclic scaffolds are reported, and properties of selected compounds discussed.
Drug Discovery and Preclinical Research, Actelion Pharmaceuticals Ltd, CH-4123 Allschwil, Switzerland.
L'ubos
L
Remen
Olivier
O
Bezençon
Sylvia
S
Richard-Bildstein
Daniel
D
Bur
Lars
L
Prade
Olivier
O
Corminboeuf
Christoph
C
Boss
Corinna
C
Grisostomi
Thierry
T
Sifferlen
Panja
P
Strickner
Patrick
P
Hess
Stéphane
S
Delahaye
Alexander
A
Treiber
Thomas
T
Weller
Christoph
C
Binkert
Beat
B
Steiner
Walter
W
Fischli
D001643:Bridged Bicyclo Compounds / Q000737:chemistry / Q000145:classification* / Q000494:pharmacology*; D018360:Crystallography, X-Ray; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000145:classification* / Q000494:pharmacology*; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D000092502:Renin Inhibitors
D001643:Bridged Bicyclo Compounds; D004791:Enzyme Inhibitors; D000092502:Renin Inhibitors