SUBSTITUTED PROLYLTYROSINES SHOWING PSYCHOTROPIC ACTIVITY Russian patent published in 1997 - IPC

FIELD: chemistry of peptides. SUBSTANCE: product: substituted prolyltyrosines of the general formula R¹-X-Pro-Y-Tyr-R² where: R¹ - H, (C₄-C₈)-alkylcarbonyl, tert. -butylhydroxycarbonyl, benzoyl, phenyl-(C₁-C₃)-alkylcarbonyl, benzylhydroxycarbonyl, phenylhydroxy-(C₁-C₃)-alkylcarbonyl; R² - O-(C₁-C₃)-alkyl, NH₂, NH-(C₁-C₃)-alkyl; X - L- or D-isomer; Y - L- or D-isomer. Synthesized compounds show psychotropic activity involving neuroleptic and antidepressant ones at doses 0.4-10 mg/kg. The proposed peptides have no by-side extrapyramidal effects and toxic symptoms at doses 2-3 orders above threshold ones and retain activity at oral administration. EFFECT: improved method of synthesis, enhanced effectiveness and safety. 11 cl, 8 tbl