New Anthranilic Acid Based Antagonists with High Affinity and Selectivity for the Human Cholecystokinin Receptor 1 (hCCK1-R)

…, L Mennuni, F Ferrari, C Escrieut, E Marco…

Index: Pavan, Michela V.; Lassiani, Lucia; Berti, Federico; Stefancich, Giorgio; Ciogli, Alessia; Gasparrini, Francesco; Mennuni, Laura; Ferrari, Flora; Escrieut, Chantal; Marco, Esther; Makovec, Francesco; Fourmy, Daniel; Varnavas, Antonio Journal of Medicinal Chemistry, 2011 , vol. 54, # 16 p. 5769 - 5785

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Citation Number: 4

Abstract

The anthranilic acid diamides represent the most recent class of nonpeptide CCK1 receptor (CCK1-R) antagonists. Herein we describe the second phase of the anthranilic acid C- terminal optimization using nonproteinogenic amino acids containing a phenyl ring in their side chain. The Homo-Phe derivative 2 (VL-0797) enhanced 12-fold the affinity for the rat CCK1-R affinity and 15-fold for the human CCK1-R relative to the reference compound 12 ...

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