| abstract |
The present invention relates to new compounds which act as specific inhibitors of the cysteine protease dipeptidyl peptidase I (DP I). These compounds are represented by the general formula AB-NHO-C, in which A can be any N-terminally unprotected amino acid other than proline and hydroxyproline, in the present case in peptide bond with B, B can be any amino acid other than proline, hydroxyproline or alanine and NHO that Hydroxylamine grouping, present in the amide bond with B and present in the ester bond with C, and C can be acyl radicals of the general formula CO-R, where R is preferably benzoyl radicals with substituents in the ortho, meta or para position or combinations of substituents in these positions, preferably which represents atoms or groupings F, Cl, Br, NO¶2¶, NH¶2¶, CH¶3¶, CH¶3¶O. DOLLAR A Compounds of this type as inhibitors of DP I are distinguished by the fact that they are chemically stable in aqueous solutions, including biological liquids. Immediately after enzymatic action by DP I on these compounds, they develop their inhibitory activity towards the target enzyme, which ultimately leads to the efficient and complete inhibition of DP I. DOLLAR A Dipeptidyl Peptidase I is known to release active, granulocytic serine proteases of lymphatic cells from their pro forms, that is to say in mechanisms which are used physiologically by cytotoxic lymphocytes in the immune system. With pathophysiological ... |