FIELD: chemistry.
SUBSTANCE: invention relates to multifunctional conjugates of tacrine and its analogues with 1,2,4-thiadiazole derivatives of general formula I, where R may be halogen, lower alkyl groups, lower alkoxy groups, trihalomethyl, acyl groups; X represents -(CH3)C = CH- or -(CH3)CHCH2-; n = 1–4; m = 2–7. Compounds of formula I are obtained by condensation of 3-(2-oxopropyl)-5-anilino-1,2,4-thiadiazole and aminoalkyl derivatives of tacrine and its analogues, followed, if necessary, by reduction of the double bond of the enamine fragment under the action of sodium borohydride when heated. Compounds of the invention are intended for use in medicine for the treatment of neurodegenerative diseases.
(I).
EFFECT: compounds are effective inhibitors of acetylcholinesterase and human butyrylcholinesterase, able to bind to the peripheral anionic site of acetylcholinesterase, bind free radicals, also as NMDA receptor blockers.
8 cl, 4 tbl, 2 dwg, 20 ex
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