| 摘要 |
organic chemistry, biochemistry, medicine, pharmacy. SUBSTANCE: invention relates to derivatives of 5-aroylnaphthalene of the formula (I) where A means -CH2-, -C(O)- or -S(O)2-; Z means group of the formula (B): or (D): where X means O or S; R6 and R7 are taken independently each of other from the group comprising hydrogen atom, C1-C6-alkyl, CF3, C1-C6-alkylthio-group, C1-C6-alkoxy-group, halogen atom, nitro-group, hydroxy-group and -NR9R10 where R9 and R10 mean independently each of other hydrogen atom or C1-C6-alkyl; R1 means hydrogen atom, C1-C6-alkyl, C1-C6-alkoxy-group, hydroxy-C2-C6-alkoxy-group, hydroxy-group, halogen atom, cyano-group, carboxy-group, OCH2CON(CH3)2,-CONR9R10,-OCONR9R10 or -OSO2R11 where R9 and R10 have values indicated above and R11 means C1-C6-alkyl or CF3/ ; R3 means -SO2R12 or -SO2NR13R14 where R12 means C1-C6-alkyl; R13 means hydrogen atom or C1-C6- alkyl and R14 means hydrogen atom, C1-C6-alkyl, C3-C6-cycloalkyl, C2-C6-alkenyl, hydroxy-C2-C6-alkyl, C1-C6-alkoxy-C1-C6-alkyl, C1-C6-alkoxy-carbonyl-C1-C6-alkyl, benzyl, phenethyl, naphthylethyl, acyl, morpholino-C1-C6-alkyl, pyrrolidinone-C1-C6-alkyl, pyridyl-C1-C6-alkyl, furanyl-C1-C6-alkyl, or R13 and R14 in common with nitrogen atom to which they are bound form optionally heterocycloamino-group taken among piperidino-, morpholino-, di-(C1-C6-alkyl)-morpholino, pyrrolidino-, methylpiperazino-, phenylpiperazino- and fluorophenylpiperazino-group; and their pharmaceutically acceptable salts or their esters or carbamates, individual isomers and isomer mixtures and to a method of their synthesis. Compounds of the formula (I) show an inhibitory activity with respect to an enzymatic activity of prostaglandin G/H synthase I and II (COX I and COX II) and show an anti-inflammatory and analgetic activity and can be used for preparing a medicinal preparation with an anti-inflammatory effect. EFFECT: compounds indicated above, improved method of synthesis, valuable medicinal properties. 20 cl, 8 tbl
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