Antsans Iu E, Bisenietse D A, Vosekalna I A, Myshliakova N V, Chipens G I
Bioorg Khim. 1990 Mar;16(3):358-69.
Five angiotensin cycloanalogues have been synthesised by classical methods of peptide chemistry, cyclisation being carried out via pentafluorophenyl esters. Cycloanalogues (I-IV) with a fixed potential turn in the C-terminal part of the angiotensin molecule inferred on the basis of physico-chemical data do not possess angiotensin-like activity. Compounds (V) with enlarged cycle shows decreased pressor effects as compared with angiotensin. By means of circular dichroism chiroptical properties of the compounds in water and ethanol were examined.
通过肽化学经典方法合成了五种血管紧张素环类似物,环化反应通过五氟苯基酯进行。根据物理化学数据推断,在血管紧张素分子C端部分具有固定潜在转角的环类似物(I-IV)不具有血管紧张素样活性。与血管紧张素相比,具有扩大环的化合物(V)显示出降低的升压作用。借助圆二色性研究了化合物在水和乙醇中的手性光学性质。