Citation: Mei Ren, Yun Gen Xu, Na Wen, Da Yong Zhang, Wei Yi Hua. Synthesis and NHE1 inhibitory activity of ligustrazine derivatives[J]. Chinese Chemical Letters, ;2007, 18(5): 539-541. doi: 10.1016/j.cclet.2007.03.020 shu

Synthesis and NHE1 inhibitory activity of ligustrazine derivatives

Mei Ren ^a, ,
Yun Gen Xu ^a ,
Na Wen ^b ,
Da Yong Zhang ^a ,
Wei Yi Hua ^a

a Center of Drug Discovery, China Pharmaceutical University, Nanjing 210009, China;
b Department of Pharmacology, China Pharmaceutical University, Nanjing 210009, China

Received Date: 29 December 2006

A series of novel derivatives of ligustrazine linked with substituted benzoyl guanidine were synthesized. These compounds have not been reported in literature, and their chemical structures were confirmed by IR, ¹H NMR and MS. The results of NHE1 inhibitory activity test showed that compounds Ⅰ₂, Ⅰ₃, Ⅰ₄, Ⅰ₆, and Ⅰ₇ possess more potent NHEl inhibitory activity than cariporide.
- Na⁺/H⁺ exchanger inhibitors,
- Ligustrazine derivatives,
- Benzoyl guanidine derivatives,
- Synthesis
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