Literature DB >> 11992786

Identification of potent and selective oxytocin antagonists. Part 1: indole and benzofuran derivatives.

Paul G Wyatt1, Michael J Allen, Josie Chilcott, Alison Foster, David G Livermore, Jackie E Mordaunt, Jan Scicinski, Patrick M Woollard.   

Abstract

Studies to discover novel, potent and selective oxytocin antagonists are reported. Combinatorial libraries designed to find novel replacements of fragments of oxytocin antagonist L-371,257, identified pyrimidine, thiazole, indole and benzofuran as potential alternatives to the benzoic acid moiety of L-371,257. Additional investigations identified indole and benzofuran derivatives with potent oxytocin antagonist activity.

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Year:  2002        PMID： 11992786     DOI： 10.1016/s0960-894x(02)00159-2

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


  3 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

2.  Possible dynamic anchor points in a benzoxazinone derivative-human oxytocin receptor system--a molecular docking and dynamics calculation.

Authors:  Balázs Jójárt; Arpád Márki
Journal:  J Mol Model       Date:  2006-05-05       Impact factor: 1.810

Review 3.  REVIEW: Oxytocin: Crossing the bridge between basic science and pharmacotherapy.

Authors:  Cedric Viero; Izumi Shibuya; Naoki Kitamura; Alexei Verkhratsky; Hiroaki Fujihara; Akiko Katoh; Yoichi Ueta; Hans H Zingg; Alexandr Chvatal; Eva Sykova; Govindan Dayanithi
Journal:  CNS Neurosci Ther       Date:  2010-07-07       Impact factor: 5.243
  3 in total

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