Aim: Over the years, indole has proved to be a versatile scaffold for the design of molecules acting as anti-inflammatory agents. Materials & Methods: A small library of 3-amino-alkylated indoles has been obtained by an optimized Mannich green approach. The anti-inflammatory activity of the new 3-amino-alkylated indoles, GLYC 0-10, was evaluated in RAW 264.7 macrophages. Results: The anti-inflammatory activity of the new 3-amino-alkylated indoles, GLYC 0-10, was evaluatedn and, among them, GLYC 4, 5 and 9 displayed the greatest inhibitory effects on nitric oxide production, with IC50 values of 5.41, 4.22 and 6.3 μM, respectively. Conclusion: Our outcomes, overall, highlight the importance of the indole substitution in the anti-inflammatory activity of these compounds, exerted by acting on the interlinked NF-κB/ERK1/2 pathways.

Mazzotta, S., Frattaruolo, L., Brindisi, M., Ulivieri, C., Vanni, F., Brizzi, A., et al. (2019). 3-Amino-alkylated indoles: Unexplored green products acting as anti-inflammatory agents. FUTURE MEDICINAL CHEMISTRY, 12(1), 5-17 [10.4155/fmc-2019-0234].

3-Amino-alkylated indoles: Unexplored green products acting as anti-inflammatory agents

Ulivieri C.;Vanni F.;Brizzi A.;Carullo G.
;
2019-01-01

Abstract

Aim: Over the years, indole has proved to be a versatile scaffold for the design of molecules acting as anti-inflammatory agents. Materials & Methods: A small library of 3-amino-alkylated indoles has been obtained by an optimized Mannich green approach. The anti-inflammatory activity of the new 3-amino-alkylated indoles, GLYC 0-10, was evaluated in RAW 264.7 macrophages. Results: The anti-inflammatory activity of the new 3-amino-alkylated indoles, GLYC 0-10, was evaluatedn and, among them, GLYC 4, 5 and 9 displayed the greatest inhibitory effects on nitric oxide production, with IC50 values of 5.41, 4.22 and 6.3 μM, respectively. Conclusion: Our outcomes, overall, highlight the importance of the indole substitution in the anti-inflammatory activity of these compounds, exerted by acting on the interlinked NF-κB/ERK1/2 pathways.
Mazzotta, S., Frattaruolo, L., Brindisi, M., Ulivieri, C., Vanni, F., Brizzi, A., et al. (2019). 3-Amino-alkylated indoles: Unexplored green products acting as anti-inflammatory agents. FUTURE MEDICINAL CHEMISTRY, 12(1), 5-17 [10.4155/fmc-2019-0234].
File in questo prodotto:
File Dimensione Formato  
FutureMedChem2019.pdf

non disponibili

Descrizione: Post-print
Tipologia: PDF editoriale
Licenza: NON PUBBLICO - Accesso privato/ristretto
Dimensione 1.64 MB
Formato Adobe PDF
1.64 MB Adobe PDF   Visualizza/Apri   Richiedi una copia

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/11365/1107432