Title of article
Synthesis of conformationally constrained analogues of KN62, a potent antagonist of the P2X7-receptor
Author/Authors
Pier Giovanni Baraldi، نويسنده , , Romeo Romagnoli، نويسنده , , Mojgan Aghazadeh Tabrizi، نويسنده , , Simonetta Falzoni، نويسنده , , Francesco Di Virgilio، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2000
Pages
4
From page
681
To page
684
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.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2000
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
790714
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