Optimization of a tertiary alcohol series of phosphodiesterase-4 (PDE4) inhibitors: Structure-activity relationship related to PDE4 inhibition and human ether-a-go-go related gene potassium channel binding affinity

Journal of Medicinal Chemistry

Volumn 46, Issue 12, 2003, Pages 2413-2426

  Friesen, Richard W ^a   Ducharme, Yves ^a   Ball, Richard G ^b   Blouin, Marc ^a   Boulet, Louise ^a   Côté, Bernard ^a   Frenette, Richard ^a   Girard, Mario ^a   Guay, Daniel ^a   Huang, Zheng ^a   Jones, Thomas R ^a   Laliberté, France ^a   Lynch, Joseph J ^b   Mancini, Joseph ^a   Martins, Evelyn ^a   Masson, Paul ^a   Muise, Eric ^a   Pon, Douglas J ^a   Siegl, Peter K S ^b   Styhler, Angela ^a   Tsou, Nancy N ^b   Turner, Mervyn J ^a   Young, Robert N ^a   Girardt, Yves ^a   more..

^a MERCK FROSST CENTRE FOR THERAPEUTIC RESEARCH   (Canada)

^b MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 [2 [3 (CYCLOPENTYLOXY) 4 METHOXYPHENYL] 2 PHENYLETHYL]PYRIDINE; CILOMILAST; L 869298; PHOSPHODIESTERASE IV INHIBITOR; POTASSIUM CHANNEL; TUMOR NECROSIS FACTOR ALPHA; UNCLASSIFIED DRUG;

ANIMAL MODEL; ARTICLE; BINDING AFFINITY; BINDING KINETICS; CONTROLLED STUDY; CYTOKINE PRODUCTION; DOG; DRUG BLOOD LEVEL; DRUG POTENCY; DRUG TOLERABILITY; ENZYME INHIBITION; GUINEA PIG; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; IN VITRO STUDY; IN VIVO STUDY; INHIBITION KINETICS; LUNG FUNCTION; NONHUMAN; QT INTERVAL; REACTION OPTIMIZATION; SQUIRREL MONKEY; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS;

3',5'-CYCLIC-NUCLEOTIDE PHOSPHODIESTERASE; ALCOHOLS; ANIMALS; BRONCHOCONSTRICTION; CRYSTALLOGRAPHY, X-RAY; CYCLIC N-OXIDES; DOGS; ELECTROCARDIOGRAPHY; ETHER-A-GO-GO POTASSIUM CHANNELS; GUINEA PIGS; HUMANS; LONG QT SYNDROME; PHOSPHODIESTERASE INHIBITORS; POTASSIUM CHANNELS; POTASSIUM CHANNELS, VOLTAGE-GATED; PROTEIN BINDING; PYRIDINES; RATS; SAIMIRI; SHEEP; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; TUMOR NECROSIS FACTOR-ALPHA; VOMITING;

EID: 12444292790     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm0204542     Document Type: Article

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