Literature DB >> 18032036

The discovery of GSK221149A: a potent and selective oxytocin antagonist.

John Liddle1, Michael J Allen, Alan D Borthwick, David P Brooks, David E Davies, Richard M Edwards, Anne M Exall, Chris Hamlett, Wendy R Irving, Andrew M Mason, Gerald P McCafferty, Fabrizio Nerozzi, Simon Peace, Joanne Philp, Derek Pollard, Mark A Pullen, Shaila S Shabbir, Steve L Sollis, Timothy D Westfall, Pat M Woollard, Charlene Wu, Deirdre M B Hickey.   

Abstract

Optimisation of a series of oxazole diketopiperazines has led to the discovery of a very potent and selective oxytocin antagonist GSK221149A. GSK221149A has been shown to inhibit oxytocin-induced uterine contractions in the anaesthetised rat.

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Year:  2007        PMID: 18032036     DOI: 10.1016/j.bmcl.2007.11.008

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


  21 in total

Review 1.  Chemistry and biology of multicomponent reactions.

Authors:  Alexander Dömling; Wei Wang; Kan Wang
Journal:  Chem Rev       Date:  2012-03-22       Impact factor: 60.622

Review 2.  Combinatorial chemistry: oh what a decade or two can do.

Authors:  Walter H Moos; Clarence R Hurt; Guillermo A Morales
Journal:  Mol Divers       Date:  2009-03-03       Impact factor: 2.943

3.  Special issue on Mini-MCR issue and SCS-09--Second International Symposium on Combinatorial Sciences in Biology, Chemistry, Catalysts and Materials. Editorial.

Authors:  Alexander Dömling; Christopher Hulme
Journal:  Mol Divers       Date:  2011-02       Impact factor: 2.943

4.  Synthesis of α-amino-1,3-dicarbonyl compounds via Ugi flow chemistry reaction: access to functionalized 1,2,3-triazoles.

Authors:  Stanley N S Vasconcelos; Evelin Fornari; Ignez Caracelli; Hélio A Stefani
Journal:  Mol Divers       Date:  2017-07-12       Impact factor: 2.943

Review 5.  Expanding the medicinal chemistry synthetic toolbox.

Authors:  Jonas Boström; Dean G Brown; Robert J Young; György M Keserü
Journal:  Nat Rev Drug Discov       Date:  2018-08-24       Impact factor: 84.694

6.  Treatment of spontaneous preterm labour with retosiban: a phase 2 proof-of-concept study.

Authors:  Steven Thornton; Hugh Miller; Guillermo Valenzuela; Jerry Snidow; Brendt Stier; Michael J Fossler; Timothy H Montague; Marcy Powell; Kathleen J Beach
Journal:  Br J Clin Pharmacol       Date:  2015-06-01       Impact factor: 4.335

7.  Concise Two-Step Solution Phase Syntheses of four novel Dihydroquinazoline scaffolds.

Authors:  Justin Dietrich; Christine Kaiser; Nathalie Meurice; Christopher Hulme
Journal:  Tetrahedron Lett       Date:  2010-07-28       Impact factor: 2.415

8.  Polycyclic compounds by Ugi-Pictet-Spengler sequence.

Authors:  Wei Wang; Sarah Ollio; Eberhardt Herdtweck; Alexander Dömling
Journal:  J Org Chem       Date:  2010-12-29       Impact factor: 4.354

9.  Efficient assembly of iminodicarboxamides by a "truly" four-component reaction.

Authors:  Kareem Khoury; Mantosh K Sinha; Tadamichi Nagashima; Eberhardt Herdtweck; Alexander Dömling
Journal:  Angew Chem Int Ed Engl       Date:  2012-09-11       Impact factor: 15.336

10.  Various cyclization scaffolds by a truly Ugi 4-CR.

Authors:  Mantosh K Sinha; Kareem Khoury; Eberhardt Herdtweck; Alexander Dömling
Journal:  Org Biomol Chem       Date:  2013-06-13       Impact factor: 3.876

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