Discovery of PF-184563, a potent and selective V1a antagonist for the treatment of dysmenorrhoea. the influence of compound flexibility on microsomal stability

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 19, 2011, Pages 5684-5687

  Johnson, Patrick S ^a   Ryckmans, Thomas ^a   Bryans, Justin ^a   Beal, Dave M ^a   Dack, Kevin N ^a   Feeder, Neil ^a   Harrison, Anthony ^a   Lewis, Mark ^a   Mason, Helen J ^a   Mills, James ^a   Newman, Julie ^a   Pasquinet, Christelle ^a   Rawson, Dave J ^a   Roberts, Lee R ^a   Russell, Rachel ^a   Spark, Deborah ^a   Stobie, Alan ^a   Underwood, Toby J ^a   Ward, Robin ^a   Wheeler, Simon ^a  

^a PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United Kingdom)

Author keywords

Lead optimisation; LiPE; Number of rotatable bonds; Triazoles; V1a antagonists

Indexed keywords

PF 184563; UNCLASSIFIED DRUG; VASOPRESSIN RECEPTOR ANTAGONIST; VASOPRESSIN V1A RECEPTOR; VASOPRESSIN V1A RECEPTOR ANTAGONIST;

ANIMAL EXPERIMENT; ARTICLE; DRUG MECHANISM; DRUG METABOLISM; DRUG POTENCY; DRUG SELECTIVITY; DYSMENORRHEA; HUMAN; LIPOPHILICITY; NONHUMAN; RAT; RAYNAUD PHENOMENON;

BENZODIAZEPINES; CYTOCHROME P-450 ENZYME SYSTEM; DRUG DESIGN; DRUG DISCOVERY; DRUG STABILITY; DYSMENORRHEA; FEMALE; HORMONE ANTAGONISTS; HUMANS; MICROSOMES; MOLECULAR STRUCTURE; RECEPTORS, VASOPRESSIN; TRIAZOLES;

EID: 80052575807     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.08.038     Document Type: Article

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