PMID

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Article Title

Organization

Cardiotonic agents. 1-Methyl-7-(4-pyridyl)-5,6,7,8-tetrahydro-3 (2H)-isoquinolinones and related compounds. Synthesis and activity.

Mitsui Toatsu Chemicals

Synthesis and structure-activity relationships of 4-oxo-1-phenyl-3,4,6,7-tetrahydro-[1,4]diazepino[6,7,1-hi]indoles: novel PDE4 inhibitors.

Institut De Recherche Jouveinal-Parke Davis

Application of structure-based drug design and parallel chemistry to identify selective, brain penetrant, in vivo active phosphodiesterase 9A inhibitors.

Pfizer

Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disorders.

Pfizer

The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases.

Monash University (Parkville Campus)

Novel, potent, and selective phosphodiesterase-4 inhibitors as antiasthmatic agents: synthesis and biological activities of a series of 1-pyridylnaphthalene derivatives.

Tanabe Seiyaku

Cyclic GMP phosphodiesterase inhibitors. 1. The discovery of a novel potent inhibitor, 4-((3,4-(methylenedioxy)benzyl)amino)-6,7,8-trimethoxyquinazoline.

Eisai

Cardiotonic agents. 8. Selective inhibitors of adenosine 3',5'-cyclic phosphate phosphodiesterase III. Elaboration of a five-point model for positive inotropic activity.

Warner-Lambert

A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity.

TBA

1,7- and 2,7-naphthyridine derivatives as potent and highly specific PDE5 inhibitors.

Tanabe Seiyaku

Synthesis of 4-(8-benzo[1,2,5]oxadiazol-5-yl-[1,7]naphthyridine-6-yl)-benzoic acid: a potent and selective phosphodiesterase type 4D inhibitor.

Novartis Pharma

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

Pfizer

Design, synthesis, and biological evaluation of 3-[4-(2-hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one, a potent, orally active, brain penetrant inhibitor of phosphodiesterase 5 (PDE5).

Pfizer

Optimization of the aminopyridopyrazinones class of PDE5 inhibitors: discovery of 3-[(trans-4-hydroxycyclohexyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one.

Pfizer

Identification of a brain penetrant PDE9A inhibitor utilizing prospective design and chemical enablement as a rapid lead optimization strategy.

Pfizer

 

Imidazotriazinone inhibitors of the Ca²⁺-calmodulin sensitive phosphodiesterase (PDE I)

TBA

The discovery of potent, selective, and orally bioavailable PDE9 inhibitors as potential hypoglycemic agents.

Pfizer

Identification of phosphodiesterase-1 and 5 dual inhibitors by a ligand-based virtual screening optimized for lead evolution.

Sumitomo Pharmaceuticals

A new chemical tool for exploring the physiological function of the PDE2 isozyme.

Pfizer

Discovery of hydroxamic acid analogs as dual inhibitors of phosphodiesterase-1 and -5.

Sumitomo Pharmaceuticals

Comparison of different heterocyclic scaffolds as substrate analog PDE5 inhibitors.

Bayer Healthcare

Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 2: Optimization of 5,8-disubstituted derivatives.

Pfizer

Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 1.

Pfizer

Discovery of thiadiazoles as a novel structural class of potent and selective PDE7 inhibitors. Part 1: design, synthesis and structure-activity relationship studies.

Pfizer

New substituted triaza-benzo[cd]azulen-9-ones as promising phosphodiesterase-4 inhibitors.

Pfizer

1-Arylnaphthalene lignan: a novel scaffold for type 5 phosphodiesterase inhibitor.

Tanabe Seiyaku

Aryl sulfonamides as selective PDE4 inhibitors.

Chiroscience

Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine.

Smithkline Beecham Pharmaceuticals

Cardiotonic agents. 1. 4,5-Dihydro-6-[4-(1H-imidazol-1-yl)phenyl]-3 (2H)-pyridazinones: novel positive inotropic agents for the treatment of congestive heart failure.

TBA

Cardiotonic agents. 5. 1,2-Dihydro-5-[4-(1H-imidazol-1-yl)phenyl]-6-methyl-2-oxo-3- pyridinecarbonitriles and related compounds. Synthesis and inotropic activity.

TBA

Cardiotonic agents. 7. Inhibition of separated forms of cyclic nucleotide phosphodiesterase from guinea pig cardiac muscle by 4,5-dihydro-6-[4-(1H-imidazol-1-yl)phenyl]-3(2H)-pyridazinones and related compounds. Structure-activity relationships and correlation with in vivo positive inotropic activi

Warner-Lambert

Structure-based design of caspase-1 inhibitor containing a diphenyl ether sulfonamide.

Pfizer