| abstract |
The invention relates to heterocyclic substances, in particular the preparation of amino acid derivatives of the total C 6 H 5 -CH 2 -CH 2 -CHK-NHCHX-C (O) -Y, where K is C (O) OR 1 n n n X - (CH 2 ) 4 -NH 2 n n n Y is NAC (O) OH where R 1 is H or C 2 H 5 n n n A - group: @ or their acid additive salts with hypotensive and cardioprotective effects, which can be used in medicine. The goal is to create new, more active substances of the specified class. The synthesis is carried out by reacting the compound YH, with the corresponding amino acid, and in the group Y, the carboxyl is protected by C 1 -C 4 alkyl, in the presence of a condensing agent, followed by deprotection of the protective groups by saponification. The desired product is isolated either in free form or in the form of the desired salt. For new compounds, a 50% inhibition of the activity of the enzyme converting angiotensin is achieved at a lower concentration of the substance than in the known case, i.e. (1.4 . 10 -8 -7.6 . 10 -8 ) - (2.9 . 10 -9 -3.5 . 10 -9 ) versus 7 . 10 -6 for enalapril. 1 tab. |