Literature DB >> 10762053

Synthesis of conformationally constrained analogues of KN62, a potent antagonist of the P2X7-receptor.

P G Baraldi1, R Romagnoli, M A Tabrizi, S Falzoni, F di Virgilio.   

Abstract

Conformationally constrained analogues of KN62 containing 1,2,3,4-tetrahydro-7-hydroxyisoquinoline-3-carboxylic acid with S configuration in position 3 were synthesized and their antagonist activities were tested on human macrophage cells. While KN62 is a potent antagonist of the P2X7 receptor, these analogues were inactive as antagonists and only one compound showed appreciable activity as P2X7 antagonist, which was 30 times weaker than that reported for KN62.

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Year:  2000        PMID： 10762053     DOI： 10.1016/s0960-894x(00)00083-4

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


  7 in total

1.  P2X7 receptors in rat brain: presence in synaptic terminals and granule cells.

Authors:  Maria Teresa Miras-Portugal; Miguel Díaz-Hernández; Lisandro Giráldez; Cristina Hervás; Rosa Gómez-Villafuertes; Raquel P Sen; Javier Gualix; Jesús Pintor
Journal:  Neurochem Res       Date:  2003-10       Impact factor: 3.996

2.  Potent P2X7 Receptor Antagonists: Tyrosyl Derivatives Synthesized Using a Sequential Parallel Synthetic Approach.

Authors:  R Gnana Ravi; Sylvia B Kertesy; George R Dubyak; Kenneth A Jacobson
Journal:  Drug Dev Res       Date:  2001-12-14       Impact factor: 4.360

3.  Identification and characterization of a novel variant of the human P2X(7) receptor resulting in gain of function.

Authors:  Chengqun Sun; Jessica Chu; Sarita Singh; Russell D Salter
Journal:  Purinergic Signal       Date:  2009-10-17       Impact factor: 3.765

4.  Negative regulation of CFTR activity by extracellular ATP involves P2Y2 receptors in CFTR-expressing CHO cells.

Authors:  B Marcet; V Chappe; P Delmas; M Gola; B Verrier
Journal:  J Membr Biol       Date:  2003-07-01       Impact factor: 1.843

5.  Reduced expression of P2Y1 receptors in connexin43-null mice alters calcium signaling and migration of neural progenitor cells.

Authors:  Eliana Scemes; Nathalie Duval; Paolo Meda
Journal:  J Neurosci       Date:  2003-12-10       Impact factor: 6.167

6.  Synthesis and structure-activity relationship studies of tyrosine-based antagonists at the human P2X7 receptor.

Authors:  Ga Eun Lee; Bhalchandra V Joshi; Wangzhong Chen; Lak Shin Jeong; Hyung Ryong Moon; Kenneth A Jacobson; Yong-Chul Kim
Journal:  Bioorg Med Chem Lett       Date:  2007-11-28       Impact factor: 2.823

7.  P2X(7) receptor: Death or life?

Authors:  Elena Adinolfi; Cinzia Pizzirani; Marco Idzko; Elisabeth Panther; Johannes Norgauer; Francesco Di Virgilio; Davide Ferrari
Journal:  Purinergic Signal       Date:  2005-07-29       Impact factor: 3.765
  7 in total

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