Synthesis of novel indole based scaffolds holding pyrazole ring as anti-inflammatory and antioxidant agents

Vishwanath Sharath , Honnaiah Vijay Kumar , Nagaraja Naik
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引用次数: 21

Abstract

Aim

To synthesize substituted indole based scaffolds having pyrazole ring and evaluate for their anti-inflammatory activity and antioxidant.

Method

The structures of newly synthesized compounds were elucidated by spectroscopic methods such as IR, 1H NMR, 13C NMR, mass, 1H NMR spectra and elemental analysis. Antioxidant assays like 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, 2,2-azino bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS+) radical ion decolorization assay and lipid peroxidation activity (LPO) were performed. Anti-inflammatory activity was studied using linoleic acid as substrate and lipoxidase enzyme.

Results

Among the synthesized analogues compound 7d revealed broad-spectrum of antioxidant activity and on the other hand compound 7c exhibits a promising anti-inflammatory activity.

Conclusion

The achieved results prove that the distinctive compounds could serve as promising lead candidates and also for acclimatization and investigation to construct more active analogues.

Abstract Image

新型吡唑环吲哚基抗炎抗氧化支架的合成
目的合成具有吡唑环的取代吲哚基支架,并评价其抗炎和抗氧化活性。方法采用IR、1H NMR、13C NMR、质谱、1H NMR和元素分析等光谱方法对新合成化合物的结构进行鉴定。进行了2,2-二苯基-1-吡啶肼基(DPPH)自由基清除、2,2-氮基双(3-乙基苯并噻唑-6-磺酸)(ABTS+)自由基脱色和脂质过氧化活性(LPO)等抗氧化实验。以亚油酸为底物,用脂氧化酶对其抗炎活性进行了研究。结果化合物7d具有广谱抗氧化活性,化合物7c具有较好的抗炎活性。结论这些独特的化合物可作为有前途的先导化合物,并可用于驯化和研究构建更有活性的类似物。
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