Discovery of triazolopyrimidine-based PDE8B inhibitors: Exceptionally ligand-efficient and lipophilic ligand-efficient compounds for the treatment of diabetes

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 17, 2012, Pages 5721-5726

  Deninno, Michael P ^a,b   Wright, Stephen W ^a   Etienne, John B ^a   Olson, Thanh V ^a   Rocke, Benjamin N ^a   Corbett, Jeffrey W ^a   Kung, Daniel W ^a   Dirico, Kenneth J ^a   Andrews, Kim M ^a   Millham, Michele L ^a   Parker, Janice C ^a   Esler, William ^a   Van Volkenburg, Maria ^a   Boyer, David D ^a   Houseknecht, Karen L ^a,c   Doran, Shawn D ^a  

^a PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United States)

^b VERTEX PHARMACEUTICALS   (United States)

^c UNIVERSITY OF NEW ENGLAND   (United States)

Author keywords

Diabetes; Ligand efficiency; Lipophilic ligand efficiency; PDE8B; Phosphodiesterase 8B

Indexed keywords

ANTIDIABETIC AGENT; PHOSPHODIESTERASE; PHOSPHODIESTERASE 8B INHIBITOR; PHOSPHODIESTERASE INHIBITOR; PYRIMIDINE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; DIABETES MELLITUS; DRUG BIOAVAILABILITY; DRUG POTENCY; DRUG SELECTIVITY; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; LIPOPHILICITY; NONHUMAN; RAT;

3',5'-CYCLIC-AMP PHOSPHODIESTERASES; ANIMALS; CELLS, CULTURED; DIABETES MELLITUS; DRUG DISCOVERY; ENZYME INHIBITORS; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; INSULIN; ISLETS OF LANGERHANS; LIGANDS; MICROSOMES, LIVER; PROTEIN BINDING; PYRIMIDINES; RATS; STRUCTURE-ACTIVITY RELATIONSHIP; TRIAZOLES;

EID: 84865149965     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.06.079     Document Type: Article

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