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

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

BARALDI, Pier Giovanni;ROMAGNOLI, Romeo;AGHAZADEH TABRIZI, Mojgan;FALZONI, Simonetta;DI VIRGILIO, Francesco
2000

Abstract

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
2000
Baraldi, Pier Giovanni; Romagnoli, Romeo; AGHAZADEH TABRIZI, Mojgan; Falzoni, Simonetta; DI VIRGILIO, Francesco
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/516474
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