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

[ Vol. 1 , Issue. 5 ]

Author(s):

A. Varnavas, L. Lassiani, V. Valenta, A. Ciogli, F. Gasparrini, L. Mennuni and F. Makovec   Pages 501 - 517 ( 17 )

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.

Keywords:

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

Affiliation:

Department of Pharmaceutical Sciences, University of Trieste, P.le Europa 1, 34127 Trieste, Italy.



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