tekturna and aliskiren

tekturna has been researched along with aliskiren* in 1 studies

Other Studies

1 other study(ies) available for tekturna and aliskiren

Article	Year
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. Journal of medicinal chemistry, 2007, Oct-04, Volume: 50, Issue:20 Due to its function in the rate limiting initial step of the renin-angiotensin system, renin is a particularly promising target for drugs designed to control hypertension, a growing risk to health worldwide. Despite vast efforts over more than two decades, no orally efficacious renin inhibitor had reached the market. As a result of a structure-based topological design approach, we have identified a novel class of small-molecule inhibitors with good oral blood-pressure lowering effects in primates. Further lead optimization aimed for improvement of in vivo potency and duration of action, mainly by P2' modifications at the hydroxyethylene transition-state isostere. These efforts resulted in the discovery of aliskiren (46, CGP060536B, SPP100), a highly potent, selective inhibitor of renin, demonstrating excellent efficacy in sodium-depleted marmosets after oral administration, with sustained duration of action in reducing dose-dependently mean arterial blood pressure. Aliskiren has recently received regulatory approval by the U.S. Food and Drug Administration for the treatment of hypertension. Topics: Administration, Oral; Amides; Animals; Antihypertensive Agents; Blood Pressure; Callithrix; Caprylates; Crystallography, X-Ray; Fumarates; Heart Rate; Humans; Kinetics; Models, Molecular; Molecular Structure; Protein Binding; Renin; Stereoisomerism; Structure-Activity Relationship	2007

Article

Year

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.

Journal of medicinal chemistry, 2007, Oct-04, Volume: 50, Issue:20

Due to its function in the rate limiting initial step of the renin-angiotensin system, renin is a particularly promising target for drugs designed to control hypertension, a growing risk to health worldwide. Despite vast efforts over more than two decades, no orally efficacious renin inhibitor had reached the market. As a result of a structure-based topological design approach, we have identified a novel class of small-molecule inhibitors with good oral blood-pressure lowering effects in primates. Further lead optimization aimed for improvement of in vivo potency and duration of action, mainly by P2' modifications at the hydroxyethylene transition-state isostere. These efforts resulted in the discovery of aliskiren (46, CGP060536B, SPP100), a highly potent, selective inhibitor of renin, demonstrating excellent efficacy in sodium-depleted marmosets after oral administration, with sustained duration of action in reducing dose-dependently mean arterial blood pressure. Aliskiren has recently received regulatory approval by the U.S. Food and Drug Administration for the treatment of hypertension.

Topics: Administration, Oral; Amides; Animals; Antihypertensive Agents; Blood Pressure; Callithrix; Caprylates; Crystallography, X-Ray; Fumarates; Heart Rate; Humans; Kinetics; Models, Molecular; Molecular Structure; Protein Binding; Renin; Stereoisomerism; Structure-Activity Relationship

2007