A set of 1-methyl-2-(4-X-benzoyl)imidazole-5 acetic acids that are structurally related to tolmetin and zomepirac were synthesized and biologically evaluated for their antiinflammatory activity. The results of in vivo tests and enzymatic assays showed that some of the investigated compounds are characterized by an analgesic-antiinflammatory profile similar or better than that of tolmetin. Preliminary structure-activity relationships suggest that activity is promoted by electron-releasing substituents in the para-position of the benzoyl moiety.
Synthesis and Structure-Activity Relationships of Antiinflammatory 1-Methyl-2-(4-X-benzoyl)imidazole-5-acetic Acids / Caliendo, Giuseppe; Cirino, Giuseppe; Greco, Giovanni; Novellino, Ettore; Perissutti, Elisa; Pinto, A.; Santagada, Vincenzo; Silipo, Carlo; Sorrentino, Ludovico. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - STAMPA. - 29:(1994), pp. 381-388. [10.1016/0223-5234(94)90063-9]
Synthesis and Structure-Activity Relationships of Antiinflammatory 1-Methyl-2-(4-X-benzoyl)imidazole-5-acetic Acids.
CALIENDO, GIUSEPPE;CIRINO, GIUSEPPE;GRECO, GIOVANNI;NOVELLINO, ETTORE;PERISSUTTI, ELISA;SANTAGADA, VINCENZO;SILIPO, CARLO;SORRENTINO, LUDOVICO
1994
Abstract
A set of 1-methyl-2-(4-X-benzoyl)imidazole-5 acetic acids that are structurally related to tolmetin and zomepirac were synthesized and biologically evaluated for their antiinflammatory activity. The results of in vivo tests and enzymatic assays showed that some of the investigated compounds are characterized by an analgesic-antiinflammatory profile similar or better than that of tolmetin. Preliminary structure-activity relationships suggest that activity is promoted by electron-releasing substituents in the para-position of the benzoyl moiety.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
