2,5-Diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists. 3. Synthesis, pharmacokinetics, and in vivo potency

Journal of Medicinal Chemistry

Volumn 49, Issue 14, 2006, Pages 4159-4170

  Borthwick, Alan D ^a   Davies, Dave E ^a   Exall, Anne M ^a   Hatley, Richard J D ^a   Hughes, Jennifer A ^a   Irving, Wendy R ^a   Livermore, David G ^a   Sollis, Steve L ^a   Nerozzi, Fabrizio ^a   Valko, Klara L ^c   Allen, Michael J ^b   Perren, Marion ^b   Shabbir, Shalia S ^a   Woollard, Patrick M ^a   Price, Mark A ^b  

^a Cell Biology Unit   (United Kingdom)

^b GLAXOSMITHKLINE   (United Kingdom)

^c GlaxoSmithKline ^*  (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

1 [1 [4 (1 ACETYL 4 PIPERIDINYLOXY) 2 METHOXYBENZOYL] 4 PIPERIDINYL]BENZ[D][1,3]OXAZIN 2 ONE; 2 (2,4 DIFLUOROPHENYL) 2 [3 (2,3 DIHYDRO 1H INDEN 2 YL) 6 (2 METHYLPROPYL) 2,5 DIOXO 1 PIPERAZINYL] N,N DIMETHYLETHANAMIDE; ATOSIBAN; CYTOCHROME P450; OXYTOCIN ANTAGONIST; PIPERAZINEDIONE; UNCLASSIFIED DRUG; VASOPRESSIN V1 RECEPTOR; VASOPRESSIN V2 RECEPTOR;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DOG; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG POTENCY; DRUG SAFETY; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; GENOTOXICITY; LIPOPHILICITY; NONHUMAN; RAT;

ADMINISTRATION, ORAL; ANIMALS; BINDING, COMPETITIVE; BIOLOGICAL AVAILABILITY; CALCIUM SIGNALING; CHO CELLS; CRICETINAE; CRICETULUS; DOGS; HUMANS; INDENES; OXYTOCIN; PIPERAZINES; RADIOLIGAND ASSAY; RATS; RECEPTORS, OXYTOCIN; RECEPTORS, VASOPRESSIN; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; UTERINE CONTRACTION;

EID: 33745868370     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm060073e     Document Type: Article

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