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Structural modification of the P2' position of 2,7-dialkyl-substituted 5(S)-amino-4(S)-hydroxy-8-phenyl-octanecarboxamides: the discovery of aliskiren, a potent nonpeptide human renin inhibitor active after once daily dosing in marmosets.
J Med Chem. 2007 Oct 4;50(20):4832-44. doi: 10.1021/jm070316i. Epub 2007 Sep 8.
J Med Chem. 2007.
PMID: 17824680
Structure-based design of aliskiren, a novel orally effective renin inhibitor.
Wood JM, Maibaum J, Rahuel J, Grütter MG, Cohen NC, Rasetti V, Rüger H, Göschke R, Stutz S, Fuhrer W, Schilling W, Rigollier P, Yamaguchi Y, Cumin F, Baum HP, Schnell CR, Herold P, Mah R, Jensen C, O'Brien E, Stanton A, Bedigian MP.
Wood JM, et al. Among authors: goschke r.
Biochem Biophys Res Commun. 2003 Sep 5;308(4):698-705. doi: 10.1016/s0006-291x(03)01451-7.
Biochem Biophys Res Commun. 2003.
PMID: 12927775
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Novel 2,7-dialkyl-substituted 5(S)-amino-4(S)-hydroxy-8-phenyl-octanecarboxamide transition state peptidomimetics are potent and orally active inhibitors of human renin.
Göschke R, Stutz S, Rasetti V, Cohen NC, Rahuel J, Rigollier P, Baum HP, Forgiarini P, Schnell CR, Wagner T, Gruetter MG, Fuhrer W, Schilling W, Cumin F, Wood JM, Maibaum J.
Göschke R, et al.
J Med Chem. 2007 Oct 4;50(20):4818-31. doi: 10.1021/jm070314y. Epub 2007 Sep 8.
J Med Chem. 2007.
PMID: 17824679
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Structure-based drug design: the discovery of novel nonpeptide orally active inhibitors of human renin.
Rahuel J, Rasetti V, Maibaum J, Rüeger H, Göschke R, Cohen NC, Stutz S, Cumin F, Fuhrer W, Wood JM, Grütter MG.
Rahuel J, et al. Among authors: goschke r.
Chem Biol. 2000 Jul;7(7):493-504. doi: 10.1016/s1074-5521(00)00134-4.
Chem Biol. 2000.
PMID: 10903938
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Synthesis and biological activity of some transition-state inhibitors of human renin.
Bühlmayer P, Caselli A, Fuhrer W, Göschke R, Rasetti V, Rüeger H, Stanton JL, Criscione L, Wood JM.
Bühlmayer P, et al. Among authors: goschke r.
J Med Chem. 1988 Sep;31(9):1839-46. doi: 10.1021/jm00117a027.
J Med Chem. 1988.
PMID: 3137345
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