Indolyl and dihydroindolyl N-glycinamides as potent and in vivo active NPY5 antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 6, 2012, Pages 2167-2171

  Wu, Lingyun ^a   Lu, Kai ^a   Packiarajan, Mathivanan ^a   Jubian, Vrej ^a   Chandrasena, Gamini ^a   Wolinsky, Toni C ^b   Walker, Mary W ^b  

^a Chemical and Pharmacokinetic Sciences   (United States)

^b LUNDBECK RESEARCH USA   (United States)

Author keywords

Brain penetration; Dihydroindolyl glycinamide; Indolyl glycinamide; PGP efflux

Indexed keywords

ANTIOBESITY AGENT; DIHYDROINDOLYL N GLYCINAMIDE DERIVATIVE; DRUG METABOLITE; GLYCINAMIDE; INDOLYL N GLYCINAMIDE DERIVATIVE; NEUROPEPTIDE Y RECEPTOR ANTAGONIST; NEUROPEPTIDE Y5 RECEPTOR; NEUROPEPTIDE Y5 RECEPTOR ANTAGONIST; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; DOSE RESPONSE; DRUG ACTIVITY; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG CLEARANCE; DRUG HALF LIFE; DRUG METABOLISM; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SCREENING; DRUG SYNTHESIS; FEEDING; FOOD INTAKE; HUMAN; IN VIVO STUDY; LIVER MICROSOME METABOLISM; MALE; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; PLASMA CLEARANCE; RAT; STRUCTURE ACTIVITY RELATION; TIME TO MAXIMUM PLASMA CONCENTRATION;

AMIDES; ANIMALS; APPETITE STIMULANTS; BRAIN; CELL LINE; EATING; GLYCINE; HUMANS; INDOLES; KINETICS; MALE; MOLECULAR STRUCTURE; PERMEABILITY; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, NEUROPEPTIDE Y; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84857918644     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.01.117     Document Type: Article

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