Synthesis and PTP1B inhibition of 1,2-naphthoquinone derivatives as potent anti-diabetic agents

被引:67
作者
Ahn, JH [1 ]
Cho, SY [1 ]
Ha, JD [1 ]
Chu, SY [1 ]
Jung, SH [1 ]
Jung, YS [1 ]
Baek, JY [1 ]
Choi, IK [1 ]
Shin, EY [1 ]
Kang, SK [1 ]
Kim, SS [1 ]
Cheon, HG [1 ]
Yang, SD [1 ]
Choi, JK [1 ]
机构
[1] Korea Res Inst Chem Technol, Div Med Sci, Taejon 305600, South Korea
关键词
D O I
10.1016/S0960-894X(02)00331-1
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A new series of 1,2-naphthoquinone derivatives was synthesized by various synthetic methods and evaluated for their ability to inhibit protein tyrosine phosphatase 1B (PTP1B). 1, 2-Naphthoquinone derivatives with substituent at R-4 position showed submicromolar inhibitory activity, and compound 24 demonstrated 10- to 60-fold selectivity against the tested phosphatases. Also, several 4-aryl-1,2-naphthoquinone derivatives with substituents at R-3, R-6, R-7, or/and R-8 showed submicromolar inhibitory activity and good plasma stability. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1941 / 1946
页数:6
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