Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 13, 2008, Pages 3716-3719

  McAtee, John J ^a   Dodson, Jason W ^a   Dowdell, Sarah E ^a   Erhard, Karl ^a   Girard, Gerald R ^a   Goodman, Krista B ^a   Hilfiker, Mark A ^a   Jin, Jian ^a   Sehon, Clark A ^a   Sha, Deyou ^a   Shi, Dongchuan ^a   Wang, Feng ^a   Wang, Gren Z ^a   Wang, Ning ^a   Wang, Yonghui ^a   Viet, Andrew Q ^a   Yuan, Catherine C K ^a   Zhang, Daohua ^a   Aiyar, Nambi V ^a   Behm, David J ^a   Carballo, Luz H ^b   Evans, Christopher A ^a   Fries, Harvey E ^a   Nagilla, Rakesh ^a   Roethke, Theresa J ^a   Xu, Xiaoping ^a   Douglas, Stephen A ^a   Neeb, Michael J ^a   more..

^a GLAXOSMITHKLINE   (United States)

^b Mathematical and Information Science Directorate Army Research Office   (United States)

Author keywords

7 TM; 7 Transmembrane; Antagonist; GPR 14; HUT; HUT II; Urotensin; UT

Indexed keywords

2 PYRROLIDINYLMETHYL 3 PHENYL PIPERIDINE; AMIDE; AMINE; BATRACHOTOXIN; CYTOCHROME P450 2D6; DIAMINE; ETHANE; ETHYLAMINE; KAPPA OPIATE RECEPTOR; KAPPA OPIATE RECEPTOR ANTAGONIST; MORPHOLINE; N METHYL 2 (1 PYRROLIDINYL)ETHANAMINE; PIPERIDINE; PIPERIDINE DERIVATIVE; PROLINE DERIVATIVE; SODIUM CHANNEL; UROTENSIN II;

ARTICLE; BINDING AFFINITY; DRUG BIOAVAILABILITY; DRUG POTENCY; DRUG STRUCTURE; ENANTIOMER; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; NONHUMAN; PROTEIN FOLDING; STEREOCHEMISTRY;

ADMINISTRATION, ORAL; ANIMALS; BRAIN; CHEMISTRY, PHARMACEUTICAL; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; DIAMINES; DRUG DESIGN; HUMANS; INHIBITORY CONCENTRATION 50; MODELS, CHEMICAL; RATS; RECEPTORS, OPIOID, KAPPA; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; UROTENSINS;

RATTUS;

EID: 44849120712     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.05.058     Document Type: Article

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