The synthesis of N-benzyl-2-chloroindole-3-carboxylic acids related to indomethacin is reported. These compounds were tested on in vitro human neutrophil activation. Some of them, more soluble in water, were tested to define the influence on prostaglandin biosynthesis via inhibition of cyclooxygenases (COX1 and COX2) by a chemiluminescent method suitable for fast screening. Several derivatives showed inhibitory effects and in some cases were more active than the parent compound.

N-Benzyl-2-chloroindole-3-carboxylic acids as potential anti-inflammatory agents. Synthesis and screening for the effects on human neutrophil functions and on COX1/COX2 activity

TRANIELLO, Maria Serena
Penultimo
;
SPISANI, Susanna
Ultimo
2004

Abstract

The synthesis of N-benzyl-2-chloroindole-3-carboxylic acids related to indomethacin is reported. These compounds were tested on in vitro human neutrophil activation. Some of them, more soluble in water, were tested to define the influence on prostaglandin biosynthesis via inhibition of cyclooxygenases (COX1 and COX2) by a chemiluminescent method suitable for fast screening. Several derivatives showed inhibitory effects and in some cases were more active than the parent compound.
Andreani, A; Granaiola, M; Leoni, A; Locatelli, A; Morigi, R; Rambaldi, M; Roda, A; Guardigli, M; Traniello, Maria Serena; Spisani, Susanna
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/1210165
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