FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to the substituted carboxamides of the formula (I)
where R1 - mercapto-, acetylthio-, carboxy-, hydroxycarbamoyl-, C1-4-alkoxycarbonyl-, ar-(C1-4)-alkoxycarbonyl-, benzylhydroxy- -carbamoyl-group or -PO(OH)-CH2SR6 where R6 means quinolyl-, naphthyl-, pyridyl- or phenyl-group; R2 means alkyl, cycloalkyl-C1-4-alkyl or aralkyl; R3 means cycloalkyl-C1-4-alkyl possibly substituted with hydroxy-, alkylthio-, pyridyl or indolyl-group; R4 means nitro-, amino-, cyano-, hydroxy-, alkoxy-, alkoxycarbonylalkyl-, tetrazolyl-, carbamoyl-group; R4 - 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
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Authors
Dates
1999-06-27—Published
1994-11-03—Filed