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Chalcones and Bis-Chalcones Analogs as DPPH and ABTS Radical Scavengers
Letters in Drug Design & Discovery ( IF 1 ) Pub Date : 2021-02-28 , DOI: 10.2174/1570180817999201001155032
Adebayo Tajudeen Bale 1 , Uzma Salar 2 , Khalid Mohammed Khan 1 , Sridevi Chigurupati 3 , Tolulope Fasina 4 , Farman Ali 1 , Muhammad Ali 1 , Sitansu Sekhar Nanda 5 , Muhammad Taha 6 , Shahnaz Perveen 7
Affiliation  

Background: A number of synthetic scaffolds, along with natural products, have been identified as potent antioxidants. The present study deals with the evaluation of varyingly substituted, medicinally distinct class of compounds “chalcones and bis-chalcones” for their antioxidant potential.

Methods: In vitro radical scavenging activities were performed on a series of synthetic chalcones 1- 13 and bis-chalcones 14-18.

Results: All molecules 1-18 revealed a pronounced 2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2ʹ- azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radicals scavenging potential in the ranges of IC50s = 0.58 ± 0.14 - 1.72 ± 0.03 and 0.49 ± 0.3 - 1.48 ± 0.06 μM, respectively. Ascorbic acid (IC50s = 0.5 ± 0.1 and 0.46 ± 0.17 μM for DPPH and ABTS, respectively) was used as a standard radical scavenger.

Conclusion: Structure-activity relationship (SAR) revealed an active participation of various groups, including -SMe and -OMe in scavenging activity.



中文翻译:

Chalcones和Bis- Chalcones类似物,作为DPPH和ABTS自由基清除剂

背景:许多合成支架以及天然产物已被确认为有效的抗氧化剂。本研究涉及对不同取代的,医学上不同的一类化合物“查耳酮和双查耳酮”的抗氧化潜力进行评估。

方法:对一系列合成查耳酮1-13和双查耳酮14-18进行体外自由基清除活性。

结果:所有分子1-18均显示出在IC 50s范围内有明显的2-二苯基-1-吡啶并肼基(DPPH)和2,2′-叠氮基双(3-乙基苯并噻唑啉-6-磺酸)(ABTS)清除自由基的能力。分别为0.58±0.14-1.72±0.03和0.49±0.3-1.48±0.06μM。抗坏血酸(DPPH和ABTS的IC 50s分别为0.5±0.1和0.46±0.17μM)用作标准自由基清除剂。

结论:结构-活性关系(SAR)显示了包括-SMe和-OMe在内的各个组的清除活性。

更新日期:2021-04-19
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