Literature DB >> 11392542

Structure-activity relationship investigations of a potent and selective benzodiazepine oxytocin antagonist.

P G Wyatt1, M J Allen, J Chilcott, G Hickin, N D Miller, P M Woollard.   

Abstract

We have investigated the structure-activity relationships of the 1- and 3-substituents and replacements of the 5-phenyl group of GW405212X 1, a potent selective oxytocin antagonist. The effect of these modifications on oxytocin binding antagonism and on pharmacokinetic parameters is reported.

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Year:  2001        PMID: 11392542     DOI: 10.1016/s0960-894x(01)00202-5

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  The 3D structure of the binding pocket of the human oxytocin receptor for benzoxazine antagonists, determined by molecular docking, scoring functions and 3D-QSAR methods.

Authors:  Balázs Jójárt; Tamás A Martinek; Arpád Márki
Journal:  J Comput Aided Mol Des       Date:  2005-05       Impact factor: 3.686

  1 in total

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