A. Varnavas, L. Lassiani, V. Valenta, A. Ciogli, F. Gasparrini, L. Mennuni and F. Makovec Pages 501 - 517 ( 17 )
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.
cholecystokinin, cck, receptors, anthranilic acid, phenylalanine derivatives, indole, antagonists, needle, ligands
Department of Pharmaceutical Sciences, University of Trieste, P.le Europa 1, 34127 Trieste, Italy.