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.
N-Terminal Anthranoyl-Phenylalanine Derivatives as CCK1 Receptor Antagonists: The Final Approach / A., Varnavas; L., Lassiani; V., Valenta; Ciogli, Alessia; Gasparrini, Francesco; L., Mennuni; F., Makovec. - In: MEDICINAL CHEMISTRY. - ISSN 1573-4064. - 1:5(2005), pp. 501-517. [10.2174/1573406054864070]
N-Terminal Anthranoyl-Phenylalanine Derivatives as CCK1 Receptor Antagonists: The Final Approach
CIOGLI, Alessia;GASPARRINI, Francesco;
2005
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
