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Biological Evaluation of Synthesized N‐Cinnamoyl Phenothiazine Derivatives
ChemistrySelect ( IF 2.1 ) Pub Date : 2018-12-07 , DOI: 10.1002/slct.201803221
Suresh Selvendran 1 , Brindha J 1 , Vasavi CS 2 , Punnagai Munussami 3 , Nithya Pattusamy 1 , Kaushik Chanda 4 , Balamurali MM 1 , Saravanakumar Rajendran 1
Affiliation  

N‐Cinnamoyl phenothiazines were synthesized and characterized by various spectroscopic techniques including vibrational, nuclear magnetic resonance and mass spectrometry. The potential applications of these compounds as antioxidants and antibacterials were evaluated. Compound 2 with –NO2 substituted cinnamoyl moiety in the phenothiazine ring nitrogen showed better antioxidant activity (77.8 μM for hydroxyl radicals and 85.0 μM for diphenyl picrylhydrazyl radicals). A moderate antibacterial activity (202‐330 μM) was observed for all the derivatives of phenothiazine against Gram‐positive and Gram‐negative bacteria, while the parent phenothiazine did not show any inhibitory activity up to 500 μM, indicating that the observed activity could be induced by the added cinnamoyl moiety. Nucleic acid and protein binding affinities were investigated for their applications as biomolecular probes. Both experimental and computational docking studies revealed an intercalative mode of binding with nucleic acids and 1:1 binding to bovine serum albumin.

中文翻译:

合成的N-肉桂酰基吩噻嗪衍生物的生物学评估

N-肉桂酰基吩噻嗪是通过各种光谱技术(包括振动,核磁共振和质谱法)合成和表征的。评估了这些化合物作为抗氧化剂和抗菌剂的潜在应用。化合物2与-NO 2吩噻嗪环氮中的肉桂酰基取代基显示出更好的抗氧化活性(羟基自由基为77.8μM,联苯吡啶甲基肼基自由基为85.0μM)。吩噻嗪的所有衍生物均对革兰氏阳性和革兰氏阴性细菌具有中等程度的抗菌活性(202-330μM),而母体吩噻嗪在500μM以下未显示任何抑制活性,表明所观察到的活性可能是由添加的肉桂酰基部分诱导。研究了核酸和蛋白质结合亲和力作为生物分子探针的应用。实验和计算对接研究均揭示了与核酸结合的插层模式以及与牛血清白蛋白的1:1结合。
更新日期:2018-12-07
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