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Bioorganic and Medicinal Chemistry Letters

Volumn 23, Issue 11, 2013, Pages 3438-3442

Discovery of potent, selective, bioavailable phosphodiesterase 2 (PDE2) inhibitors active in an osteoarthritis pain model, Part I: Transformation of selective pyrazolodiazepinone phosphodiesterase 4 (PDE4) inhibitors into selective PDE2 inhibitors

(26) 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 more..

a PFIZER INC (United States)

Author keywords

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

Indexed keywords

PHOSPHODIESTERASE II INHIBITOR; PHOSPHODIESTERASE INHIBITOR; PHOSPHODIESTERASE IV INHIBITOR; UNCLASSIFIED DRUG;

ALKYLATION; ARTICLE; CRYSTAL STRUCTURE; CYCLIZATION; DRUG BINDING; DRUG BIOAVAILABILITY; DRUG POTENCY; DRUG SELECTIVITY; ENZYME ACTIVE SITE; ENZYME ACTIVITY; ENZYME INHIBITION; HYDROGEN BOND; IC 50; MITSUNOBU REACTION; OSTEOARTHRITIS; STRUCTURE ACTIVITY RELATION;

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

EID: 84877583170 PISSN: 0960894X EISSN: 14643405 Source Type: Journal
DOI: 10.1016/j.bmcl.2013.03.072 Document Type: Article

Times cited : (17)

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