Literature DB >> 22018787

Synthesis and biological evaluation of novel pyrimidine derivatives as sub-micromolar affinity ligands of GalR2.

Vasudeva Naidu Sagi1, Tianyu Liu, Xiaoying Lu, Tamas Bartfai, Edward Roberts.   

Abstract

GalR1 and GalR2 represent unique pharmacological targets for treatment of seizures and epilepsy. A novel series of 2,4,6-triaminopyrimidine derivatives were synthesized and found to have sub-micromolar affinity for GalR2. Optimization of a series of 2,4,6-triaminopyrimidines led to the discovery of several analogs with IC50 values ranging from 0.3 to 1 μM. Copyright Â
© 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID： 22018787      PMCID： PMC3278223          DOI： 10.1016/j.bmcl.2011.09.033

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


  31 in total

1.  Modulation of hippocampal excitability and seizures by galanin.

Authors:  A M Mazarati; J G Hohmann; A Bacon; H Liu; R Sankar; R A Steiner; D Wynick; C G Wasterlain
Journal:  J Neurosci       Date:  2000-08-15       Impact factor: 6.167

2.  Galmic, a nonpeptide galanin receptor agonist, affects behaviors in seizure, pain, and forced-swim tests.

Authors:  Tamas Bartfai; Xiaoying Lu; Hedieh Badie-Mahdavi; Alasdair M Barr; Andrey Mazarati; Xiao-Ying Hua; Tony Yaksh; Gebhard Haberhauer; Susana Conde Ceide; Laurent Trembleau; Laszlo Somogyi; Lenz Kröck; Julius Rebek
Journal:  Proc Natl Acad Sci U S A       Date:  2004-07-06       Impact factor: 11.205

3.  Quantitative distribution of galanin-like immunoreactivity in the rat central nervous system.

Authors:  G Skofitsch; D M Jacobowitz
Journal:  Peptides       Date:  1986 Jul-Aug       Impact factor: 3.750

4.  Distribution of galaninlike immunoreactivity in the rat central nervous system.

Authors:  T Melander; T Hökfelt; A Rökaeus
Journal:  J Comp Neurol       Date:  1986-06-22       Impact factor: 3.215

5.  Isolation and characterization of a complementary DNA (galanin) clone from estrogen-induced pituitary tumor messenger RNA.

Authors:  M E Vrontakis; L M Peden; M L Duckworth; H G Friesen
Journal:  J Biol Chem       Date:  1987-12-15       Impact factor: 5.157

6.  Galanin - a novel biologically active peptide from porcine intestine.

Authors:  K Tatemoto; A Rökaeus; H Jörnvall; T J McDonald; V Mutt
Journal:  FEBS Lett       Date:  1983-11-28       Impact factor: 4.124

7.  Distribution and regulation of galanin receptor 1 messenger RNA in the forebrain of wild type and galanin-transgenic mice.

Authors:  J G Hohmann; A Juréus; D N Teklemichael; A M Matsumoto; D K Clifton; R A Steiner
Journal:  Neuroscience       Date:  2003       Impact factor: 3.590

8.  GalR2-positive allosteric modulator exhibits anticonvulsant effects in animal models.

Authors:  Xiaoying Lu; Edward Roberts; Fengcheng Xia; Manuel Sanchez-Alavez; Tianyu Liu; Roger Baldwin; Stephanie Wu; James Chang; Claude G Wasterlain; Tamas Bartfai
Journal:  Proc Natl Acad Sci U S A       Date:  2010-07-26       Impact factor: 11.205

Review 9.  The participation of galanin in pain processing at the spinal level.

Authors:  Hong-Xiang Liu; Tomas Hökfelt
Journal:  Trends Pharmacol Sci       Date:  2002-10       Impact factor: 14.819

10.  Galanin type 2 receptors regulate neuronal survival, susceptibility to seizures and seizure-induced neurogenesis in the dentate gyrus.

Authors:  Andrey Mazarati; Xiaoying Lu; Kalle Kilk; Ulo Langel; Claude Wasterlain; Tamas Bartfai
Journal:  Eur J Neurosci       Date:  2004-06       Impact factor: 3.386
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  2 in total

1.  Galanin receptors and ligands.

Authors:  Kristin E B Webling; Johan Runesson; Tamas Bartfai; Ulo Langel
Journal:  Front Endocrinol (Lausanne)       Date:  2012-12-07       Impact factor: 5.555

2.  2-[4-(Chloro-meth-yl)phen-oxy]-4,6-dimeth-oxy-pyrimidine.

Authors:  Shi-Hong Shen; Kui Hu; Li Sun; Xiao-Long Fan; Hong Dai
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-06-16
  2 in total

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