N-(膦酰基乙酰基)-二肽衍生物的合成及其降压活性评估。
Synthesis of N-(phosphonoacetyl)-dipeptide derivatives and evaluation of their antihypertensive activity.
作者信息
Osapay G, Körmöczy P, Szilágyi I, Kajtár J, Kiss B
机构信息
Research Institute of Chinoin Pharmaceutical and Chemical Works, L Eötvös University, Budapest, Hungary.
出版信息
Pharmazie. 1990 Sep;45(9):666-8.
A series of N-(phosphonoacetyl)-dipeptide derivatives was synthesized for pharmacological testing as antihypertensive compounds. Several of these compounds demonstrated a moderate antihypertensive effect in Wistar spontaneous hypertensive rats (SHR) with p.o. dosing. ACE inhibition by the compounds was studied using ACE from rat plasma and lung. Inhibitors containing esterified C-termini are pro-drugs and showed activity only for plasma ACE.
合成了一系列N-(膦酰基乙酰基)-二肽衍生物，作为抗高血压化合物进行药理测试。其中几种化合物经口服给药后，在Wistar自发性高血压大鼠（SHR）中显示出中度抗高血压作用。使用大鼠血浆和肺中的ACE研究了这些化合物对ACE的抑制作用。含有酯化C末端的抑制剂是前药，仅对血浆ACE有活性。
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