SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF ANTIINFLAMMATORY 1-METHYL-2-(4-X-BENZOYL)IMIDAZOLE-5-ACETIC ACIDS

Authors
CALIENDO G CIRINO G GRECO G NOVELLINO E PERISSUTTI E PINTO A SANTAGADA V SILIPO C SORRENTINO L
Citation
G. Caliendo et al., SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF ANTIINFLAMMATORY 1-METHYL-2-(4-X-BENZOYL)IMIDAZOLE-5-ACETIC ACIDS, European journal of medicinal chemistry, 29(5), 1994, pp. 381-388
Citations number
18
Categorie Soggetti
Chemistry Medicinal
Journal title
European journal of medicinal chemistry → ACNP
ISSN journal
02235234
Volume
29
Issue
5
Year of publication
1994
Pages
381 - 388
Database
ISI
SICI code
0223-5234(1994)29:5<381:SASOA1>2.0.ZU;2-9
Abstract
A set of 1-methyl-2-(4-X-benzoyl)imidazole-5 acetic acids that are str ucturally related to tolmetin and zomepirac were synthesized and biolo gically evaluated for their antiinflammatory activity. The results of in vivo tests and enzymatic assays showed that some of the investigate d compounds are characterized by an analgesic-antiinflammatory profile similar or better than that of tolmetin. Preliminary structure-activi ty relationships suggest that activity is promoted by electron-releasi ng substituents in the para-position of the benzoyl moiety.