Gante J, Krug M, Lauterbach G, Weitzel R, Hiller W
E. Merck Darmstadt, Medicinal Chemistry Cardiovascular Department, Germany.
J Pept Sci. 1995 May-Jun;1(3):201-6. doi: 10.1002/psc.310010307.
The synthesis of the first all-aza-amino acid analogue (2) of a peptidic renin inhibitor is described. The X-ray structural analysis and molecular modelling investigations of this novel compound reveal interesting conformational features which have a significant impact on its biological activity. In addition, insight into conformational features of azapeptides in general in comparison with the corresponding purely peptidic compounds is given.
本文描述了一种肽类肾素抑制剂的首个全氮杂氨基酸类似物（2）的合成。对这种新型化合物的X射线结构分析和分子建模研究揭示了有趣的构象特征，这些特征对其生物活性有重大影响。此外，还对氮杂肽与相应的纯肽类化合物相比的一般构象特征进行了深入探讨。
