Syntheses and Bioactivities of 4-Ar-2-oxo-glutaric Acids

被引:0
|
作者
Schofield Christopher [1 ]
机构
[1] CRL University of Oxford South Parks Road Oxford OX1 3QY UK
关键词
2-Oxo-glutaric acid; Bioactivity; Inhibitor; Synthesis;
D O I
暂无
中图分类号
TQ450.1 [基础理论];
学科分类号
090403 ;
摘要
Fourteen novel compounds were synthesized and characterized by using NMR and ESI-MS methods. The bioactivities of the four novel 4-Ar-2-oxo-glutaric acids were studied by using the LC-MS method. The experimental results show that 3-nitrobenzyl-2-oxo-glutaric acid is a mild inhibitor for the hydroxylation reaction catalyzed by PHD2. The decarboxylated peak for 3-fluorobenzyl-2-oxo-glutaric acid was observed by using the negative LC-MS method, indicating that it can be used as a mild cosubstrate to replace 2-OG, but this is possible only in the presence of the prime peptide CODD 19 mer.
引用
收藏
页码:284 / 288
页数:5
相关论文
共 50 条
  • [41] 2-, 3-, and 4-(1-Oxo-1H-2,3-dihydroisoindol-2-yl)benzoic acids and their corresponding organotin carboxylates: Synthesis, characterization, fluorescent, and biological activities
    Cai, Shuang-Lian
    Chen, Yong
    Sun, Wen-Xia
    Li, Hui
    Chen, Yun
    Yuan, Shi-Shan
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2010, 20 (19) : 5649 - 5652
  • [42] Synthesis and Fungicidal Activity of N-(2,4,5-trichlorophenyl)-2-Oxo-and 2-Hydroxycycloalkylsulfonamides
    Li, Xing-Hai
    Pan, Qiang
    Cui, Zi-Ning
    Ji, Ming-Shan
    Qi, Zhi-Qiu
    LETTERS IN DRUG DESIGN & DISCOVERY, 2013, 10 (04) : 353 - 359
  • [43] Synthesis and molecular structure of the tetranuclear μ4-oxo-centered chromium complex [Cr4(CH2CH2CH2NMe2)4(μ4-O)(μ-Cl)6]
    Ossola, F
    Benetollo, F
    JOURNAL OF ORGANOMETALLIC CHEMISTRY, 1999, 580 (01) : 56 - 59
  • [44] Synthesis and crystal Structure of spiro[1-bromo-4-methoxy-5-oxa-6-oxo-bicyclo[3.1.0]hexane-2,2′-(3′-cyclohexanoxy-4′-methoxybutyrolactone]
    Yu, ZL
    Li, SL
    Guo, JB
    Chen, QH
    CHINESE JOURNAL OF STRUCTURAL CHEMISTRY, 2005, 24 (01) : 94 - 98
  • [45] Synthesis and Crystal Structure of Spiro[1-bromo-4-methoxy-5-oxa-6-oxo-bicyclo[3.1.0]hexane-2,2′-(3′-cyclohexanoxy-4′-methoxybutyrolactone]
    YU Zhao-Lian LI Sen-Lan GUO Jin-Bo CHEN Qing-Hua② (Department of Chemistry
    Chinese Journal of Structural Chemistry, 2005, (01) : 94 - 98
  • [46] Synthesis, crystal structure and bioactivities of N-(4-methylbenzamido)-N′-[5-(2-trifluoromethylphenyl)-2-furoyl]thiourea
    Xue Si-Jia
    Bian Wang-Dong
    Chan An
    Yu Song-Rui
    CHINESE JOURNAL OF CHEMISTRY, 2008, 26 (08) : 1501 - 1505
  • [47] Efficient syntheses of 2-(2,6-dichloro-4-trifluoromethylphenyl)tetrahydrocyclopenta, tetrahydrothiopyrano, hexahydrocycloheptapyrazoles and tetrahydroindazoles
    Meegalla, SK
    Doller, D
    Liu, RP
    Sha, DY
    Soll, RM
    Dhanoa, DS
    TETRAHEDRON LETTERS, 2002, 43 (48) : 8639 - 8642
  • [48] Synthesis and Spectroscopic Studies of Lanthanide(III) Complexes with (Z)-4-OXO-4-(Phenylamino) But-2-enoic Acid
    Niu, Li-E
    Yang, Ying
    Qi, Xin-Hua
    Liang, Xing
    SYNTHESIS AND REACTIVITY IN INORGANIC METAL-ORGANIC AND NANO-METAL CHEMISTRY, 2009, 39 (01) : 1 - 5
  • [49] Syntheses of 2(3)-fluoro-4-methoxymethylbenzyl and 2(3)-fluoro-4-methylbenzyl ester of pyrethric acid and their insecticidal activity
    Zhang, QX
    Chen, Z
    Zou, XZ
    CHINESE JOURNAL OF ORGANIC CHEMISTRY, 2005, 25 (08) : 991 - 993
  • [50] Syntheses, Crystal Structures and Biological Activity of the 1D Chain Benzyltin Complexes Based on 2-Oxo-Propionic Acid Benzoyl Hydrazone
    Tan, Yu-Xing
    Zhang, Zhi-Jian
    Feng, Yong-Lan
    Yu, Jiang-Xi
    Zhu, Xiao-Ming
    Zhang, Fu-Xing
    Kuang, Dai-Zhi
    Jiang, Wu-Jiu
    JOURNAL OF INORGANIC AND ORGANOMETALLIC POLYMERS AND MATERIALS, 2017, 27 (01) : 342 - 352