Facile synthesis of some pyrazoline-based compounds with promising anti-inflammatory activity.

AIM: Search for new anti-inflammatory agents with higher efficacy and lower toxicity is an urgent demand in drug discovery era.

METHODOLOGY: Different pyrazoline derivatives 4a,b, 5a,b, 6a-h and 7a-f were prepared from the condensation reactions of 1,5-bis(5-methylfuran/thiophen-2-yl)penta-1,4-dien-3-ones 3a,b with different hydrazine derivatives. All compounds were screened for their anti-inflammatory activity using the carrageenan-induced paw edema method in rats and TNF-α inhibition assay.

RESULTS: Many compounds revealed promising anti-inflammatory activity relative to indomethacin especially compounds 4a, 5a, 5b, 6b, 6d, 6f and 7b. They were safe to the gastric mucosa and did not cause toxicity up to tenfolds the anti-inflammatory dose, in addition, all compounds inhibited TNF-α with IC50 values of 1.7-100 nM.