Investigation of aminopyridiopyrazinones as PDE5 inhibitors: Evaluation of modifications to the central ring system

Autor:	Alan MacInnes, E. Jon Jacobsen, Robert Hughes, Blevis-Bal Radhika M, Jennifer M. Williams, John K. Walker, Joseph B. Moon, Jeanne M. Rumsey, Brad A. Acker, Steve E. Heasley, Maddux Todd Michael, Dafydd R. Owen, Ying Yu, John M. Molyneaux, Jerry W. Cubbage, Brian R. Bond, Brown David L, Alan G. Benson, John N. Freskos, William C. Stallings, Brent V. Mischke, Yvette M. Fobian, D. Joseph Rogier, Yi Zheng, Mike B. Tollefson
Rok vydání:	2009
Předmět:	medicine.drug_mechanism_of_action Stereochemistry Phosphodiesterase Inhibitors Chemistry Pharmaceutical Clinical Biochemistry Pharmaceutical Science Administration Oral Aminopyridines Ring (chemistry) Biochemistry Rats Sprague-Dawley Microsomes Drug Discovery medicine Potency Animals Humans Molecular Biology Cyclic GMP Cyclic Nucleotide Phosphodiesterases Type 5 Improved solubility Chemistry Organic Chemistry Phosphoric Diester Hydrolases Metabolic stability Hydrogen-Ion Concentration Phosphodiesterase 5 Inhibitors Cyclic nucleotide phosphodiesterases Combinatorial chemistry Rats Sprague dawley Models Chemical Solubility Drug Design Pyrazines Hypertension Molecular Medicine Phosphodiesterase 5 inhibitor
Zdroj:	Bioorganicmedicinal chemistry letters. 19(15)
ISSN:	1464-3405
Popis:	Efforts to improve the potency and physical properties of the aminopyridiopyrazinone class of PDE5 inhibitors through modification of the core ring system are described. Five new ring systems are evaluated and features that impart improved potency and improved solubility are delineated.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3c530b519c26bbcf215a387ac7749266 https://pubmed.ncbi.nlm.nih.gov/19539468 Zobrazit plný text záznamu Full Text from ScienceDirect