DERIVATIVES OF N-ACYLPROLYLDIPEPTIDES Russian patent published in 1998 - IPC

FIELD: organic chemistry, chemistry of peptides. SUBSTANCE: products: derivatives of N-acylprolyldipeptides of the general formula (I): where (C⁴-C⁵) is $$4-alkyl, cycloalkyl, aralkyl or aryl; R² is H, (C¹-C⁴)-alkyl, carbamidoalkyl or carbalkoxyalkyl; R³ is hydroxy-, alkoxy-, amino-, alkylamino- or dialkylamino-group; n = 0-3 and a) when R¹ is phenyl, R² is hydrogen or isopropyl and n = 0 then R³ is not methoxy-group; b) when R¹ is tert.-butyl, R² is hydrogen and n = 0 or 1 then R³ is not methylamino-group; c) when R¹ is tert.-butyl, R² is isobutyl, methyl, benzyl or carbamidomethyl and n = 0 then R³ is not methylamino-group; d) when R¹ is tret.-butyl, R² is carbomethoxymethyl and n = 0 then R³ is not isopropylamino-group. Compounds are synthesized by condensation of the required acids in homogeneous phase at blocking no reacting functional groups using condensing agents, for example, carbodiimide. Synthesized compounds are used in medicine since they show antiamnestic, antihypoxic and anorexigeneous effects, low toxicity. Compounds of the formula (I) are able to decrease benzodiazepine withdrawal syndrome, anxiety, aggressivity and kindling induced by pentylenetetrazole. Compounds improve memory and teaching capability. EFFECT: improved method of synthesis, enhanced effectiveness of compounds synthesized. 11 cl, 14 tbl, 33 ex