| abstract |
FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to the substituted carboxamides of the formula (I) where R 1 - mercapto-, acetylthio-, carboxy-, hydroxycarbamoyl-, C 1-4 -alkoxycarbonyl-, ar-(C 1-4 )-alkoxycarbonyl-, benzylhydroxy- -carbamoyl-group or -PO(OH)-CH 2 SR 6 where R 6 means quinolyl-, naphthyl-, pyridyl- or phenyl-group; R 2 means alkyl, cycloalkyl-C 1-4 -alkyl or aralkyl; R 3 means cycloalkyl-C 1-4 -alkyl possibly substituted with hydroxy-, alkylthio-, pyridyl or indolyl-group; R 4 means nitro-, amino-, cyano-, hydroxy-, alkoxy-, alkoxycarbonylalkyl-, tetrazolyl-, carbamoyl-group; R 4 - hydrogen atom or hydroxy-group as a separate stereoisomer or their mixture, or its pharmaceutically acceptable salt that show capability to inhibit activity of matrix metalloproteases. EFFECT: improved method of synthesis, inhibitory effect of enzyme activities. 16 cl, 32 ex |