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Design and optimization of potent, selective antagonists of Oxytocin.
Brown, Alan; Brown, Lindsay; Ellis, Dave; Puhalo, Nicholas; Smith, Chris R; Wallace, Olga; Watson, Lesa.
Affiliation
  • Brown A; Discovery Chemistry, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK. Alan.D.Brown@pfizer.com
Bioorg Med Chem Lett ; 18(15): 4278-81, 2008 Aug 01.
Article in En | MEDLINE | ID: mdl-18639455
ABSTRACT
A novel series of Oxytocin antagonists are described. This series was identified through pharmacophoric overlap of in-house and literature antagonists. Subsequent optimization led to a series of potent, selective antagonists. Several analogues displayed oral bioavailability in vivo in the rat.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Oxytocics / Triazoles / Oxytocin Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2008 Type: Article Affiliation country: United kingdom
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Oxytocics / Triazoles / Oxytocin Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2008 Type: Article Affiliation country: United kingdom