Literature DB >> 16481165

Structure-activity relationship of thiopyrimidines as mGluR5 antagonists.

Lance G Hammerland1, Martin Johansson, Jonas Malmström, Jan P Mattsson, Alexander B E Minidis, Karolina Nilsson, Alecia Peterson, David Wensbo, Andreas Wållberg, Krister Osterlund.   

Abstract

Structure-activity relationship investigations of the thiopyrimidine (1), an HTS hit with micromolar activity as a metabotropic glutamate receptor 5 (mGluR5) antagonist, led to compounds with sub-micromolar activity.

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Year:  2006        PMID： 16481165     DOI： 10.1016/j.bmcl.2006.01.100

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


  5 in total

1.  Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists.

Authors:  Santosh S Kulkarni; Amy Hauck Newman
Journal:  Bioorg Med Chem Lett       Date:  2007-03-24       Impact factor: 2.823

Review 2.  Controlled microwave heating in modern organic synthesis: highlights from the 2004-2008 literature.

Authors:  C Oliver Kappe; Doris Dallinger
Journal:  Mol Divers       Date:  2009-04-21       Impact factor: 2.943

3.  Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS.

Authors:  Ya Zhou; Alice L Rodriguez; Richard Williams; C David Weaver; P Jeffrey Conn; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2009-10-28       Impact factor: 2.823

4.  5-Aryl-6-arylthio-2,2'-bipyridine and 6-Arylthio-2,5-diarylpyridine Fluorophores: Pot, Atom, Step Economic (PASE) Synthesis and Photophysical Studies.

Authors:  Maria I Savchuk; Dmitry S Kopchuk; Olga S Taniya; Igor L Nikonov; Ilya N Egorov; Sougata Santra; Grigory V Zyryanov; Oleg N Chupakhin; Valery N Charushin
Journal:  J Fluoresc       Date:  2021-05-08       Impact factor: 2.217

5.  Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype.

Authors:  Alice L Rodriguez; Richard Williams; Ya Zhou; Stacey R Lindsley; Uyen Le; Mark D Grier; C David Weaver; P Jeffrey Conn; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2009-05-03       Impact factor: 2.823
  5 in total

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