Lin W Q, Cai C Y, Gong K S, Wu Y, Long Z, Luo X X, Yang L, Li J F, Yao X J
School of Pharmacy, West China University of Medical Sciences, Chengdu.
Yao Xue Xue Bao. 1994;29(5):346-54.
This paper reports the synthesis of eleven N-(4-carbomethoxy-4-phthalimidobutanoyl)-N-substituted glycines (VII1-9), proline (VII10) and pyroglutamic acid (VII11) expected to have inhibitory activity on angiotensin converting enzyme. All of the compounds mentioned above and the corresponding t-butyl esters of VII1-9 were not reported in the literature previously. The structures were confirmed through their IR, 1HNMR, MS spectra and elemental analysis. In preliminary test in rats, compounds VII8, VII9 and VII10 showed marked hypotensive activity.
本文报道了11种预期对血管紧张素转换酶具有抑制活性的N-(4-甲氧羰基-4-邻苯二甲酰亚胺基丁酰基)-N-取代甘氨酸（VII1-9）、脯氨酸（VII10）和焦谷氨酸（VII11）的合成。上述所有化合物以及VII1-9相应的叔丁酯以前在文献中均未报道。通过红外光谱、核磁共振氢谱、质谱和元素分析对其结构进行了确证。在大鼠的初步试验中，化合物VII8、VII9和VII10表现出显著的降压活性。
