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.
2005
antagonists; anthranilic acid; cck; cck1; cholecystokinin; indole; ligands; needle; phenylalanine derivatives; receptors
01 Pubblicazione su rivista::01a Articolo in rivista
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]
File allegati a questo prodotto
Non ci sono file associati a questo prodotto.

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11573/239909
 Attenzione

Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo

Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus 4
  • ???jsp.display-item.citation.isi??? 4
social impact