Discovery of potent selective bioavailable phosphodiesterase 2 (PDE2) inhibitors active in an osteoarthritis pain model. Part II: Optimization studies and demonstration of in vivo efficacy

Bioorganic and Medicinal Chemistry Letters

Volumn 23, Issue 11, 2013, Pages 3443-3447

  Plummer, Mark S ^a   Cornicelli, Joseph ^a   Roark, Howard ^a   Skalitzky, Donald J ^a   Stankovic, Charles J ^a   Bove, Susan ^a   Pandit, Jayvardhan ^a   Goodman, Annise ^a   Hicks, James ^a   Shahripour, Aurash ^a   Beidler, David ^a   Lu, Xiao Kang ^a   Sanchez, Brian ^a   Whitehead, Christopher ^a   Sarver, Ron ^a   Braden, Timothy ^a   Gowan, Richard ^a   Shen, Xi Qiang ^a   Welch, Katherine ^a   Ogden, Adam ^a   Sadagopan, Nalini ^a   Baum, Heidi ^a   Miller, Howard ^a   Banotai, Craig ^a   Spessard, Cindy ^a   Lightle, Sandra ^a   more..

^a PFIZER INC   (United States)

Author keywords

Osteoarthritis (OA) pain; Phosphodiesterase 2 (PDE2) inhibitors; Structure based drug design

Indexed keywords

PHOSPHODIESTERASE INHIBITOR; PHOSPHODIESTERASE IV INHIBITOR; PYRAZOLODIAZEPINONE; UNCLASSIFIED DRUG;

ANALGESIC ACTIVITY; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CRYSTAL STRUCTURE; DRUG BIOAVAILABILITY; ENZYME ACTIVE SITE; IN VIVO STUDY; NONHUMAN; OSTEOARTHRITIS; OSTEOARTHRITIS PAIN; PAIN; RAT; STRUCTURE ACTIVITY RELATION;

ANALGESICS; ANIMALS; AZEPINES; AZIRINES; BINDING SITES; CATALYTIC DOMAIN; CRYSTALLOGRAPHY, X-RAY; CYCLIC NUCLEOTIDE PHOSPHODIESTERASES, TYPE 2; DIHYDROPYRIDINES; DISEASE MODELS, ANIMAL; DRUG EVALUATION, PRECLINICAL; HALF-LIFE; OSTEOARTHRITIS; PHOSPHODIESTERASE 4 INHIBITORS; PHOSPHODIESTERASE INHIBITORS; PROTEIN BINDING; PYRAZOLES; RATS; STRUCTURE-ACTIVITY RELATIONSHIP;

RATTUS;

EID: 84877579805     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2013.03.082     Document Type: Article

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