title: Investigation of the pyrazinones as PDE5 inhibitors: evaluation of regioisomeric projections into the solvent region.
abstract: 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.
authors.affiliation: Pfizer Global Research and Development, 700 Chesterfield Parkway West, St. Louis, MO 63017, USA. robowenhughes@gmail.com
authors.forename: Robert O
authors.initials: RO
authors.lastname: Hughes
authors.forename: Todd
authors.initials: T
authors.lastname: Maddux
authors.forename: D
authors.initials: D
authors.lastname: Joseph Rogier
authors.forename: Sharon
authors.initials: S
authors.lastname: Lu
authors.forename: John K
authors.initials: JK
authors.lastname: Walker
authors.forename: E
authors.initials: E
authors.lastname: Jon Jacobsen
authors.forename: Jeanne M
authors.initials: JM
authors.lastname: Rumsey
authors.forename: Yi
authors.initials: Y
authors.lastname: Zheng
authors.forename: Alan
authors.initials: A
authors.lastname: Macinnes
authors.forename: Brian R
authors.initials: BR
authors.lastname: Bond
authors.forename: Seungil
authors.initials: S
authors.lastname: Han
mesh_terms: D018360:Crystallography, X-Ray; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D058986:Phosphodiesterase 5 Inhibitors / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D011719:Pyrazines / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D012997:Solvents / Q000737:chemistry
chemical_list: D058986:Phosphodiesterase 5 Inhibitors; D011719:Pyrazines; D012997:Solvents