Synthesis of cinnamoyl ketoamides as hybrid structures of antioxidants and calpain inhibitors.

Yoo YJ; Nam DH; Jung SY; Jang JW; Kim HJ; Jin C; Pae AN; Lee YS

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Synthesis of cinnamoyl ketoamides as hybrid structures of antioxidants and calpain inhibitors.

机译：肉桂酰基酮酰胺的合成，作为抗氧化剂和钙蛋白酶抑制剂的杂化结构。

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The excessive calpain activation causes serious cellular damage or even cell death in neurological disorders such as stroke and Alzheimer's disease. Oxidative stress has also been implicated in the initiation or progression of neurodegenerative diseases. In the present studies, a series of cinnamoyl ketoamides 4a-4j were synthesized as hybrid structures of antioxidants and calpain inhibitors. Cinnamoyl ketoamides, possessing an alkyl chain at the alpha-position, showed potent mu-calpain inhibitory activities indicating that the cinnamoyl skeleton can be regarded as an acyclic variant of calpain inhibitory chromone carboxamide 2. Among synthesized, compound 4e was the most potent inhibitor of mu-calpain (IC(50)=0.13 muM) and also exhibited strong antioxidant activities in DPPH and superoxide anion radical scavenging and lipid peroxidation inhibition assay systems.

机译：钙蛋白酶的过度活化会导致严重的细胞损伤，甚至导致中风和阿尔茨海默氏病等神经系统疾病的细胞死亡。氧化应激也与神经退行性疾病的发生或发展有关。在本研究中，合成了一系列肉桂酰基酮酰胺4a-4j作为抗氧化剂和钙蛋白酶抑制剂的杂化结构。在α位具有烷基链的肉桂酰基酮酰胺显示出强大的μ-钙蛋白酶抑制活性，表明肉桂酰基骨架可被认为是钙蛋白酶抑制色酮羧酰胺2的无环变异体。在合成物中，化合物4e是最有效的抑制剂。 mu-calpain（IC（50）= 0.13μM），并且在DPPH和超氧阴离子自由基清除和脂质过氧化抑制测定系统中也显示出强大的抗氧化活性。

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《Bioorganic and Medicinal Chemistry Letters》 |2011年第10期|共5页
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Yoo YJ; Nam DH; Jung SY; Jang JW; Kim HJ; Jin C; Pae AN; Lee YS;
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1. Synthesis of cinnamoyl ketoamides as hybrid structures of antioxidants and calpain inhibitors. [J] . Yoo YJ, Nam DH, Jung SY, Bioorganic and Medicinal Chemistry Letters . 2011,第10期

机译：肉桂酰基酮酰胺的合成，作为抗氧化剂和钙蛋白酶抑制剂的杂化结构。
2. [P2V3W15O62](9-) cluster based covalent polyoxometalate-organic hybrid: Synthesis, structure, self-assembly and in vitro antioxidant activities [J] . Reddy Pulikanti Guruprasad, Satyanarayana V. S. V., Dubey Vinay, Inorganic Chemistry Communications . 2015,第Null期

机译：[P2V3W15O62]（9-）团簇基共价多金属氧酸盐-有机杂化物：合成，结构，自组装和体外抗氧化活性
3. Synthesis, Structure, and Antioxidant Activity of Hybrid N-Substituted Salicylic Acid Amides [J] . N. M. Storozhok, N. P. Medyanik, A. P. Krysin Russian Journal of Organic Chemistry . 2013,第7期

机译：杂化N-取代水杨酸酰胺的合成，结构和抗氧化活性
4. Synthesis, structural, physical and chemical characterization of hybrid magnetic liposome nanocarriers of novel antioxidants for targeted drug delivery [C] . E. Halevas, T.A. Papadopoulos, A. Hatzidimitriou, 2017 IEEE International Magnetics Conference . 2017

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5. Enzymatic Synthesis of Glycerol-Based Galloyl Structured Lipids: Characterization and Application as Antioxidants [D] . Zhang, Siyu. 2020

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6. Co-crystal structures of primed side-extending α-ketoamide inhibitors reveal novel calpain-inhibitor aromatic interactions [O] . Jin Qian, Dominic Cuerrier, Peter L. Davies, -1

机译：引发侧向延伸的α-酮酰胺抑制剂的共晶体结构揭示了新的钙蛋白酶抑制剂芳族相互作用
7. Faculty Opinions recommendation of Crystal structure of SARS-CoV-2 main protease provides a basis for design of improved α-ketoamide inhibitors. [O] . Gemma Mazzuoli-Weber, Kristin Elfers 2020

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Synthesis of cinnamoyl ketoamides as hybrid structures of antioxidants and calpain inhibitors.

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