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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. Among authors: fuhrer w. J Med Chem. 2007 Oct 4;50(20):4818-31. doi: 10.1021/jm070314y. Epub 2007 Sep 8. J Med Chem. 2007. PMID: 17824679
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.
Maibaum J, Stutz S, Göschke R, Rigollier P, Yamaguchi Y, Cumin F, Rahuel J, Baum HP, Cohen NC, Schnell CR, Fuhrer W, Gruetter MG, Schilling W, Wood JM. Maibaum J, et al. Among authors: fuhrer w. 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: fuhrer w. 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
CGP 22979A, a renal vasodilator with natriuretic properties.
Hofbauer KG, Sonnenburg C, Stalder R, Criscione L, Kraetz J, Fuhrer W, Habicht E. Hofbauer KG, et al. Among authors: fuhrer w. J Pharmacol Exp Ther. 1985 Mar;232(3):838-44. J Pharmacol Exp Ther. 1985. PMID: 3973831
13 results