Synthesis and biological evaluation of novel series of chalcone derivatives as inhibitors of eyclooxygenase and LPS-induced TNF-alpha with potent antioxidant properties

摘要

Novel series of chalcones were synthesized and were evaluated as possible anti-inflammatory agents targeting the eyclooxygenase-1 and 2 (COX-1 and 2), beta-glucu-ronidase, trypsin, and TNF-a. Amongst the tested chalcones the compound 4k was found to be most effective inhibitor of TNF-a exhibiting 85% inhibition activity (IC_50 = 0.1 muM). The compounds 4a, 4f, 41, and 4m were found to inhibit the COX-1 activity in as a range of 79.95-68.47% and COX-2 inhibition ranging 84.45-74.77%. The compounds 41 (81.71%) and 4f (72.10%) were found to be excellent inhibitors of trypsin and beta-glucuronidase, respectively.