N-Terminal Anthranoyl-Phenylalanine Derivatives as CCK1 Receptor Antagonists: The Final Approach

Title: N-Terminal Anthranoyl-Phenylalanine Derivatives as CCK1 Receptor Antagonists: The Final Approach

Volume: 1 Issue: 5

Author(s): A. Varnavas, L. Lassiani, V. Valenta, A. Ciogli, F. Gasparrini, L. Mennuni and F. Makovec

Affiliation:

Keywords: cholecystokinin, cck, receptors, anthranilic acid, phenylalanine derivatives, indole, antagonists, needle, ligands

Abstract: Starting from our lead compound, VL-0395, an anthranilic acid based CCK1 receptor antagonist, and following the well established "step by step" lead investigation strategy, we describe the final step of the anthranilic acid N-terminal optimization. Improvements for both affinity and selectivity towards CCK1 receptors have been accomplished through introduction of the fluoro substituent at C-5 and C-7 position of the indole ring together with the appropriate configuration of the aminoacidic chiral center.

Cite this article as:

Varnavas A., Lassiani L., Valenta V., Ciogli A., Gasparrini F., Mennuni L. and Makovec F., N-Terminal Anthranoyl-Phenylalanine Derivatives as CCK1 Receptor Antagonists: The Final Approach, Medicinal Chemistry 2005; 1 (5) . https://dx.doi.org/10.2174/1573406054864070