Literature DB >> 16380255

Phenyl ureas of creatinine as mGluR5 antagonists. A structure-activity relationship study of fenobam analogues.

Andreas Wållberg1, Karolina Nilsson, Krister Osterlund, Alecia Peterson, Susanne Elg, Patrick Raboisson, Udo Bauer, Lance G Hammerland, Jan P Mattsson.   

Abstract

Fenobam (1) was developed by McNeil Laboratories as an anxiolytic agent with an unknown molecular target in the late 1970s. In a recent publication, it was revealed that fenobam is a non-competitive mGluR5 antagonist. Herein, we present the structure-activity relationship of fenobam and its analogues and similarities between the SAR of mGluR5 antagonism and the SAR of CNS properties originally reported by McNeil are discussed.

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Year:  2005        PMID: 16380255     DOI: 10.1016/j.bmcl.2005.11.092

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


  7 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

2.  Sleep and diurnal rest-activity rhythm disturbances in a mouse model of Alzheimer's disease.

Authors:  Mikolaj J Filon; Eli Wallace; Samantha Wright; Dylan J Douglas; Lauren I Steinberg; Carissa L Verkuilen; Pamela R Westmark; Rama K Maganti; Cara J Westmark
Journal:  Sleep       Date:  2020-11-12       Impact factor: 5.849

3.  2-Amino-5-(3,4-dimethoxybenzylidene)-1-methylimidazol-4(5H)-one N,N-dimethylformamide monosolvate.

Authors:  Laura M Tvedte; Kenneth L Smith; Eric V Patterson; Russell G Baughman
Journal:  Acta Crystallogr C       Date:  2010-02-03       Impact factor: 1.172

4.  Synthesis and Evaluation of Metabotropic Glutamate Receptor Subtype 5 Antagonists Based on Fenobam().

Authors:  Moses G Gichinga; Jeremy P Olson; Elizabeth Butala; Hernán A Navarro; Brian P Gilmour; S Wayne Mascarella; F Ivy Carroll
Journal:  ACS Med Chem Lett       Date:  2011-10-05       Impact factor: 4.345

Review 5.  Fragile X Syndrome and Alzheimer's Disease: Another story about APP and beta-amyloid.

Authors:  J S Malter; B C Ray; P R Westmark; C J Westmark
Journal:  Curr Alzheimer Res       Date:  2010-05       Impact factor: 3.498

6.  Reversal of fragile X phenotypes by manipulation of AβPP/Aβ levels in Fmr1KO mice.

Authors:  Cara J Westmark; Pamela R Westmark; Kenneth J O'Riordan; Brian C Ray; Crystal M Hervey; M Shahriar Salamat; Sara H Abozeid; Kelsey M Stein; Levi A Stodola; Michael Tranfaglia; Corinna Burger; Elizabeth M Berry-Kravis; James S Malter
Journal:  PLoS One       Date:  2011-10-26       Impact factor: 3.240

7.  The role of water and protein flexibility in the structure-based virtual screening of allosteric GPCR modulators: an mGlu5 receptor case study.

Authors:  Zoltán Orgován; György G Ferenczy; György M Keserű
Journal:  J Comput Aided Mol Des       Date:  2019-09-21       Impact factor: 3.686

  7 in total

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