- Synthesis and anti-inflammatory activity of polyazaheterocyclic derivatives of 6-amino-2,4-lutidine and their precursors.
Synthesis and anti-inflammatory activity of polyazaheterocyclic derivatives of 6-amino-2,4-lutidine and their precursors.
Arzneimittel-Forschung (1997-05-01)
J M Robert, O Rideau, S Robert-Piessard, M Duflos, G Le Baut, N Grimaud, M Juge, J Y Petit
PMID9205778
ABSTRACT
Derivatives of N-(4,6-pyridin-2-yl)arylcarboxamides resulting from the integration of the amidic function into 4H-1,2,4-triazole, triazol-3(2H)-one and 1H-tetrazole rings were evaluated as potential anti-inflammatory compounds. The level of activity decreased as compared to carboxamides, nevertheless their precursors and notably the corresponding amidrazones exhibited potent activity; amidrazone 21, whose ID50 was 34.4 mg.kg-1 in the rat paw edema test, was selected for further investigation. These heteroarylcarboxamide derivatives could represent an interesting alternative to classical non-steroidal anti-inflammatories in so far as they partly act by inhibition of tumor necrosis factor-alpha production.