A set of 1-methyl-2-(4-X-benzoyl)imidazole-5-carboxylic acids, designed as antiinflammatory-analgesic agents, were synthesized and biologically evaluated in vivo (writhing test and the carrageenen rat pleurisy) using tolmetin as a reference drug. The compounds were also tested in vitro on the cyclooxygenase enzyme of sheep vescicular microsome. Distribution coefficients In the octanol-buffer system at different pH values have been determined for their potential influence on activity. Although the investigated compounds exhibited moderate or no inhibitory activity against cyclooxygenase in in vitro and in vivo assays, two of them (the 4-nitrobenzoyl and the 4-chlorobenzoyl derivatives 1e and 1b) were found to be more active than tolmetin in the writhing test. Moreover, 1b also showed higher activity in the pleurisy assay.

Synthesis and Antiinflammatory-Analgesic Profile of 1-Methyl-2-(4-X-benzoyl)imidazole-5-carboxylic 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. - 30:4(1995), pp. 315-320. [10.1016/0223-5234(96)88239-0]

Synthesis and Antiinflammatory-Analgesic Profile of 1-Methyl-2-(4-X-benzoyl)imidazole-5-carboxylic Acids.

CALIENDO, GIUSEPPE;CIRINO, GIUSEPPE;GRECO, GIOVANNI;NOVELLINO, ETTORE;PERISSUTTI, ELISA;SANTAGADA, VINCENZO;SILIPO, CARLO;SORRENTINO, LUDOVICO
1995

Abstract

A set of 1-methyl-2-(4-X-benzoyl)imidazole-5-carboxylic acids, designed as antiinflammatory-analgesic agents, were synthesized and biologically evaluated in vivo (writhing test and the carrageenen rat pleurisy) using tolmetin as a reference drug. The compounds were also tested in vitro on the cyclooxygenase enzyme of sheep vescicular microsome. Distribution coefficients In the octanol-buffer system at different pH values have been determined for their potential influence on activity. Although the investigated compounds exhibited moderate or no inhibitory activity against cyclooxygenase in in vitro and in vivo assays, two of them (the 4-nitrobenzoyl and the 4-chlorobenzoyl derivatives 1e and 1b) were found to be more active than tolmetin in the writhing test. Moreover, 1b also showed higher activity in the pleurisy assay.
1995
Synthesis and Antiinflammatory-Analgesic Profile of 1-Methyl-2-(4-X-benzoyl)imidazole-5-carboxylic 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. - 30:4(1995), pp. 315-320. [10.1016/0223-5234(96)88239-0]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11588/457492
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