N-terminal anthranoyl-phenylalanine derivatives as CCK1 receptor antagonists: the final approach
| Autor: | Alessia Ciogli, Francesco Gasparrini, L. Mennuni, Antonio Varnavas, F. Makovec, Valentina Valenta, Lucia Lassiani |
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| Přispěvatelé: | Varnavas, Antonio, Lassiani, Lucia, Valenta, V, Ciogli, A, Gasparrini, F, Mennuni, L, Makovec, F. |
| Rok vydání: | 2006 |
| Předmět: |
Male
Indoles Time Factors phenylalanine derivatives Stereochemistry Phenylalanine Guinea Pigs cck Substituent receptors Ring (chemistry) cck1 Rats Sprague-Dawley chemistry.chemical_compound Structure-Activity Relationship needle Drug Discovery Anthranilic acid Animals ortho-Aminobenzoates Receptor antagonists Indole test Binding Sites Molecular Structure ligands anthranilic acid cholecystokinin indole Antagonist Stereoisomerism Rats Receptor Cholecystokinin A chemistry Selectivity Lead compound CCK1 receptor |
| Zdroj: | Medicinal chemistry (Shariqah (United Arab Emirates)). 1(5) |
| ISSN: | 1573-4064 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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