03-P-113
含环丙烷的双酰肼类化合物的合成及抗氧化活性
刘幸海a ,董卫莉a ,何国荣b ,王素华a ,李正名a*
a. 南开大学元素有机化学国家重点实验室,天津300071
b. 中国医学科学院药物研究所国家新药筛选中心,北京100050
Email :
研制和开发新型抗氧化剂是医药和食品行业的研究热点之一。机体内的自由基能引起很多疾病,如癌症,动脉硬化,机体老化等。同时自由基在神经系统疾病中也扮演着重要的角色,如帕金森等。我们设计了一系列的含环丙烷的双酰肼类化合物,生物活性结果表明部分化合物具有良好的抗氧化活性。
Table 1. Radical-scavenging activity of title compounds.
232H 52H 5
1
2345Et 3N, THFN H H N R 6a-6q
R=ph, o-CH3ph, o-Clph, 2,4-Cl2ph, p-Clph, p-OCH3ph, p-NO2ph, o-Fph, o-OCH3ph,
o-OH-ph, m-CH3ph, 3,4-Cl2ph, Py, furan, iso-Py, 2,4-dimethylthiazole, n-Pr
Scheme 2 Synthesis route for compounds 3a–o
关键词:合成,双酰肼,抗氧化活性
参考文献:
[1] Ke Li, Xiaoming Li, Naiyun Ji and Bingui Wang, Bioorg Med Chem, 2007, 15, 6627-6631.
Synthesis and DPPH Radical-Scavenging Activity of Some Novel
N,N ′-diacylhydrazines
Xing-Hai Liua , Wei-Li Donga , Guo-Rong Heb , Su-Hua Wanga , *Zheng-Ming Lia a. State-Key Laboratory of Elemento-Organic Chemistry, Nankai University, Tianjin 300071;b. National Centre for Pharmaceutical Screening, Institute of Materia Mdeica,
Chinese Academy of Medical Sciences, Beijing 100050
To develop of novel Anti-oxidation reagents is an important research research topic in the field of medicine and food. Free radical attacks living organism, and leads to cell or tissue injury associated with diseases including atherosclerosis, carcinogenesis and aging. In addition, free radical-mediated oxidative-damage plays an important role as an underlying factor in the initiation and progression of some neurodegenerative disorders such as Parkinson’s diseases. A series of N,N’-diacylhydrzines were designed and synthesized, the biological activity shows some of the title compounds had excellent DPPH radical-scavenging activity. 164
03-P-113
含环丙烷的双酰肼类化合物的合成及抗氧化活性
刘幸海a ,董卫莉a ,何国荣b ,王素华a ,李正名a*
a. 南开大学元素有机化学国家重点实验室,天津300071
b. 中国医学科学院药物研究所国家新药筛选中心,北京100050
Email :
研制和开发新型抗氧化剂是医药和食品行业的研究热点之一。机体内的自由基能引起很多疾病,如癌症,动脉硬化,机体老化等。同时自由基在神经系统疾病中也扮演着重要的角色,如帕金森等。我们设计了一系列的含环丙烷的双酰肼类化合物,生物活性结果表明部分化合物具有良好的抗氧化活性。
Table 1. Radical-scavenging activity of title compounds.
232H 52H 5
1
2345Et 3N, THFN H H N R 6a-6q
R=ph, o-CH3ph, o-Clph, 2,4-Cl2ph, p-Clph, p-OCH3ph, p-NO2ph, o-Fph, o-OCH3ph,
o-OH-ph, m-CH3ph, 3,4-Cl2ph, Py, furan, iso-Py, 2,4-dimethylthiazole, n-Pr
Scheme 2 Synthesis route for compounds 3a–o
关键词:合成,双酰肼,抗氧化活性
参考文献:
[1] Ke Li, Xiaoming Li, Naiyun Ji and Bingui Wang, Bioorg Med Chem, 2007, 15, 6627-6631.
Synthesis and DPPH Radical-Scavenging Activity of Some Novel
N,N ′-diacylhydrazines
Xing-Hai Liua , Wei-Li Donga , Guo-Rong Heb , Su-Hua Wanga , *Zheng-Ming Lia a. State-Key Laboratory of Elemento-Organic Chemistry, Nankai University, Tianjin 300071;b. National Centre for Pharmaceutical Screening, Institute of Materia Mdeica,
Chinese Academy of Medical Sciences, Beijing 100050
To develop of novel Anti-oxidation reagents is an important research research topic in the field of medicine and food. Free radical attacks living organism, and leads to cell or tissue injury associated with diseases including atherosclerosis, carcinogenesis and aging. In addition, free radical-mediated oxidative-damage plays an important role as an underlying factor in the initiation and progression of some neurodegenerative disorders such as Parkinson’s diseases. A series of N,N’-diacylhydrzines were designed and synthesized, the biological activity shows some of the title compounds had excellent DPPH radical-scavenging activity. 164