N-terminal anthranoyl-phenylalanine derivatives as CCK1 receptor antagonists: the final approach
A Varnavas1, L Lassiani, V Valenta
1Department of Pharmaceutical Sciences, University of Trieste, P.le Europa 1, 34127 Trieste, Italy. varnavas@units.it
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.
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