Enzyme inhibition potency enhancement by active site metal chelating and hydrogen bonding induced conformation-restricted cyclopropanecarbonyl derivatives

PY Kuo, TL Shie, YS Chen, JT Lai, DY Yang

文献索引：Kuo, Pei-Yu; Shie, Tien-Lan; Chen, You-Sheng; Lai, Jiun-Ting; Yang, Ding-Yah Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 23 p. 6024 - 6027

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被引用次数: 9

摘要

Two cyclopropanecarbonyl derivatives were independently found to be 15 and 14 times more potent than the corresponding isopropylcarbonyl analogues as inhibitors of 4- hydroxyphenylpyruvate dioxygenase and dihydroorotate dehydrogenase, respectively. A thorough examination of the co-crystal structures of available enzyme inhibitor complexes and the conformation of X-ray crystal structures of several synthesized ...