Investigation of the pyrazinones as PDE5 inhibitors: Evaluation of regioisomeric projections into the solvent region

We describe the design, synthesis and profiling of a novel series of PDE5 inhibitors. We take advantage of an alternate projection into the solvent region to identify compounds with excellent potency, selectivity and pharmacokinetic profiles.

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2011-11, Vol.21 (21), p.6348-6352
Hauptverfasser:	Hughes, Robert O., Maddux, Todd, Joseph Rogier, D., Lu, Sharon, Walker, John K., Jon Jacobsen, E., Rumsey, Jeanne M., Zheng, Yi, MacInnes, Alan, Bond, Brian R., Han, Seungil
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences Cardiovascular system chemistry Crystallography, X-Ray Inhibitory Concentration 50 Lead optimization Ligand efficiency Lipophilic efficiency Medical sciences Miscellaneous Models, Molecular PDE5 inhibitors pharmacokinetics Pharmacology. Drug treatments Phosphodiesterase 5 Inhibitors - chemistry Phosphodiesterase 5 Inhibitors - pharmacokinetics Phosphodiesterase 5 Inhibitors - pharmacology Pyrazines - chemistry Pyrazines - pharmacokinetics Pyrazines - pharmacology Pyrazinones solvents Solvents - chemistry
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	We describe the design, synthesis and profiling of a novel series of PDE5 inhibitors. We take advantage of an alternate projection into the solvent region to identify compounds with excellent potency, selectivity and pharmacokinetic profiles.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2011.08.106