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

被引：11

作者：

Bandgar, Babasaheb P. ^{[1
,2
]}

Hote, Baliram S. ^{[2
]}

Dhole, Nagesh A. ^{[3
]}

Gacche, Rajesh N. ^{[3
]}

机构：

[1] Solapur Univ, Med Chem Res Lab, Sch Chem Sci, Solapur, Maharashtra, India

[2] SRTM Univ, Organ Chem Res Lab, Sch Chem Sci, Nanded, Maharashtra, India

[3] SRTM Univ, Biochem Res Lab, Sch Life Sci, Nanded, Maharashtra, India

来源：

MEDICINAL CHEMISTRY RESEARCH | 2012年 / 21卷 / 09期

关键词：

WBCs; TNF-alpha; COX-1; COX-2; Antioxidant; Enzyme inhibition; ANTIINFLAMMATORY ACTIVITY; FLAVONOIDS;

D O I：

10.1007/s00044-011-9746-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Novel series of chalcones were synthesized and were evaluated as possible anti-inflammatory agents targeting the cyclooxygenase-1 and 2 (COX-1 and 2), beta-glucuronidase, trypsin, and TNF-alpha. Amongst the tested chalcones the compound 4k was found to be most effective inhibitor of TNF-alpha exhibiting 85% inhibition activity (IC50 = 0.1 mu M). The compounds 4a, 4f, 4l, 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 4l (81.71%) and 4f (72.10%) were found to be excellent inhibitors of trypsin and beta-glucuronidase, respectively.

引用

页码：2292 / 2299

页数：8

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