Total synthesis and antihypertensive activity of (±)7,8-dihydroxy-3-methyl-isochromanone-4

被引:28
作者
Liu, Jie [1 ]
Ren, Hao [1 ]
Xu, Jinyi [1 ]
Bai, Renren [1 ]
Yan, Qi [1 ]
Huang, Wenlong [2 ]
Wu, Xiaoming [2 ]
Fu, Jihua [3 ]
Wang, Qiujuan [3 ]
Wu, Qian [3 ]
Fu, Rong [3 ]
机构
[1] China Pharmaceut Univ, Dept Med Chem, Nanjing 210009, Peoples R China
[2] China Pharmaceut Univ, Ctr Drug Discovery, Nanjing 210038, Peoples R China
[3] China Pharmaceut Univ, Dept Physiol, Nanjing 210009, Peoples R China
关键词
(+/-)7,8-Dihydroxy-3-methyl-isochromanone-4; Total synthesis; Antihypertensive activity; ACE inhibitors;
D O I
10.1016/j.bmcl.2008.12.102
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
This letter describes the total synthesis, preliminary biological evaluation and mechanism studies of a novel and structurally unique isochromanone, (+/-)7,8-dihydroxy-3-methyl-isochromanone-4 (1), a nature product contained in banana (Musa sapientum L.) peel. The bioassay showed that compound 1 displays potent antihypertensive activity in renal hypertensive rats and further mechanism studies revealed that it is an ACE inhibitor. (C) 2008 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1822 / 1824
页数:3
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