Bioorganic & medicinal chemistry

A new type of carboxypeptidase A inhibitors designed using an imidazole as a zinc coordinating ligand

KJ Lee, KC Joo, EJ Kim, M Lee, DH Kim

文献索引：Lee, Kyung Joo; Joo, Keum Chan; Kim, Eun-Jung; Lee, Mijoon; Kim, Dong H. Bioorganic and Medicinal Chemistry, 1997 , vol. 5, # 10 p. 1989 - 1998

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被引用次数: 23

摘要

2-(4-Imidazoyl) hydrocinnamic acid (1) and its congeners (2–4) having different length of alkyl chain spacers between the imidazole ring and the α-carbon to the carboxylate of 1 have been designed, synthesized and evaluated as inhibitors for carboxypeptidase A to show that they are competitive inhibitors for the enzyme. Inhibitor 1 was most potent having the Ki value of 0.8 μM. The present study demonstrates that imidazole ring is an effective ...