Literature DB >> 19819046

Substituted 2-aminothiopen-derivatives: a potential new class of GluR6-antagonists.

D Briel1, A Rybak, C Kronbach, K Unverferth.   

Abstract

In the course of search for new therapeutic agents against epilepsy new inhibitors for the kainate receptor subtypes GluR5 and GluR6 were synthesized. We were able to synthesize new substituted thieno[2,3-d]pyrimidines 3a,b, 4a,b, 5a,b as well as thiophene-3-carboxamides 2a-d and a multitude of substituted 4-methyl-5-phenylthiophene-3-carboxylic acids. All compounds described herein were tested for their antagonistic effect towards the kainate receptor subtypes GluR5 and GluR6. The highest activity was observed for ethyl 2-amino-4-methyl-5-phenylthiophene-3-carboxylate 1c with an IC50=0.75 microM at the GluR6 receptor. Copyright 2009 Elsevier Masson SAS. All rights reserved.

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Year:  2009        PMID： 19819046     DOI： 10.1016/j.ejmech.2009.09.025

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN： 0223-5234            Impact factor:   6.514


  6 in total

1.  Design, synthesis and biological evaluations of N-Hydroxy thienopyrimidine-2,4-diones as inhibitors of HIV reverse transcriptase-associated RNase H.

Authors:  Jayakanth Kankanala; Karen A Kirby; Andrew D Huber; Mary C Casey; Daniel J Wilson; Stefan G Sarafianos; Zhengqiang Wang
Journal:  Eur J Med Chem       Date:  2017-09-28       Impact factor: 6.514

2.  Alchemical Design of Pharmacological Chaperones with Higher Affinity for Phenylalanine Hydroxylase.

Authors:  María Conde-Giménez; Juan José Galano-Frutos; María Galiana-Cameo; Alejandro Mahía; Bruno L Victor; Sandra Salillas; Adrián Velázquez-Campoy; Rui M M Brito; José Antonio Gálvez; María D Díaz-de-Villegas; Javier Sancho
Journal:  Int J Mol Sci       Date:  2022-04-19       Impact factor: 6.208

3.  Reassignment of the structures of products produced by reactions of the product believed to be 2-(1-phenyl-2-thiocyanatoethylidene)-malononitrile with electrophiles.

Authors:  Saleh Mohammed Al-Mousawi; Moustafa Sherief Moustafa; Mohamed Hilmy Elnagdi
Journal:  Molecules       Date:  2011-04-26       Impact factor: 4.411

4.  Studies on 3-oxoalkanenitriles: novel rearrangement reactions observed in studies of the chemistry of 3-heteroaroyl-3-oxoalkanenitriles as novel routes to 2-dialkylaminopyridines.

Authors:  Hamad M Al-Matar; Khaled D Khalil; Mona F Al-Kanderi; Mohamed H Elnagdi
Journal:  Molecules       Date:  2012-01-18       Impact factor: 4.411

5.  2-Amino-4,5-dihydrothiophene-3-carbonitriles: A New Synthesis, Quantum Chemical Studies, and Mannich-Type Reactions Leading to New Hexahydrothieno[2,3-d]pyrimidines.

Authors:  Victor V Dotsenko; Alexander V Bespalov; Arthur S Vashurin; Nicolai A Aksenov; Inna V Aksenova; Elena A Chigorina; Sergey G Krivokolysko
Journal:  ACS Omega       Date:  2021-11-19

6.  An efficient synthesis of N-substituted 3-nitrothiophen-2-amines.

Authors:  Sundaravel Vivek Kumar; Shanmugam Muthusubramanian; J Carlos Menéndez; Subbu Perumal
Journal:  Beilstein J Org Chem       Date:  2015-09-22       Impact factor: 2.883
  6 in total

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