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Synthesis and properties of the first all-aza analogue of a biologically active peptide
J Gante1, M Krug, G Lauterbach
1E. Merck Darmstadt, Medicinal Chemistry Cardiovascular Department, Germany.
Abstract:
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.