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.
Remen
L'ubos
L
Drug Discovery and Preclinical Research, Actelion Pharmaceuticals Ltd, CH-4123 Allschwil, Switzerland.
Bezençon
Olivier
O
Richard-Bildstein
Sylvia
S
Bur
Daniel
D
Prade
Lars
L
Corminboeuf
Olivier
O
Boss
Christoph
C
Grisostomi
Corinna
C
Sifferlen
Thierry
T
Strickner
Panja
P
Hess
Patrick
P
Delahaye
Stéphane
S
Treiber
Alexander
A
Weller
Thomas
T
Binkert
Christoph
C
Steiner
Beat
B
Fischli
Walter
W
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