The discovery and synthesis of highly potent subtype selective phosphodiesterase 4D inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 18, 2010, Pages 5502-5505

  Aspiotis, Renee ^a   Deschênes, Denis ^a   Dubé, Daniel ^a   Girard, Yves ^a   Huang, Zheng ^a   Laliberté, France ^a   Liu, Susana ^a   Papp, Robert ^a   Nicholson, Donald W ^a   Young, Robert N ^a  

^a MERCK FROSST CENTRE FOR THERAPEUTIC RESEARCH   (Canada)

Author keywords

Asthma; COPD; PDE4D; Phosphodiesterase 4D inhibitors; Quinoline

Indexed keywords

ANTINEOPLASTIC AGENT; CILOMILAST; L 454560; NICOTINAMIDE; NVP ABE171; PHOSPHODIESTERASE IV INHIBITOR; QUINOLINE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; IC 50; MALE; NONHUMAN; PROSTATE CANCER; RAT; STRUCTURE ACTIVITY RELATION; TISSUE DISTRIBUTION;

ANIMALS; ASTHMA; CYCLIC NUCLEOTIDE PHOSPHODIESTERASES, TYPE 4; HUMANS; INHIBITORY CONCENTRATION 50; MALE; PHOSPHODIESTERASE INHIBITORS; QUINOLINES; RATS; RATS, WISTAR; STRUCTURE-ACTIVITY RELATIONSHIP;

RATTUS;

EID: 77956170810     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.07.076     Document Type: Article

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39. Compound 26b was administered separately to male Wistar-Han rats at 3 mg/kg by oral gavage, 3 mg/kg interperitoneally and 1 mg/kg intravenously. Plasma samples were collected in EDTA tubes at specified time-points up to 24 h postdose. The plasma samples were extracted using protein precipitation. Tissue samples were homogenized in water using a bead beating device and aliquots extracted by protein precipitation with acetonitrile. All bioanalytical measurements were made using a ThermoFisher Transcend LX2 Parallel UHPLC system (Franklin, MA, USA) coupled to an Applied Biosystems API4000 triple quadrupole mass spectrometer (Foster City, CA, USA). Standards and quality controls were prepared in the corresponding blank tissue matrix.