Studies on post-angioplastic restenosis have shown the implication of angiotensin I1 (Ang) as a myoproliferative mediator. The antiproliferative efficacy of non-peptide Ang antagonists on the rat carotid model is of 50%, whereas a continuously infused peptide antagonist at low doses totally blocks neointimal growth. To explore the feasibility of depot forms of Ang that may be introduced during angioplasty and thus prevent restenosis, lipid-masked Ang analogues of the following general structure were prepared :

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Lipid Masking and Reactivation of Angiotensin Analogues.-A number of lipid-masked angiotensin analogues such as (I) are prepared in order to find new molecular tools against post-angioplastic restenosis. S-and O-acylated Ser and Cys peptides like ( Ic) are found to be unstable. They easily undergo transacylation giving N-acylated peptides. Biologically inactive S-and O-acylated peptides can easily be hydrolyzed and, thus, transformed to their biologically active form, whereas N-acylated analogues are not easily cleavable. -(MALETINSKA, L.; NEUGEBAUER, W.; PARE, M.-C.; PERODIN, J.; PHAM, D.; ESCHER, E.; Helv.