Patent AT-E400179-T1: [Translated] USE OF PYRIMIDINETRION DERIVATIVES AS ACETYLCHOLINESTERASE INHIBITORS, COMPOSITIONS CONTAINING SAME AND USES THEREOF

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Pyrimidine derivatives (I) are used as acetylcholinesterase inhibitors. Pyrimidine derivatives of formula (I) are used as acetylcholinesterase inhibitors. R 1, R 3 = H or optionally unsaturated 1-6C (cyclo)alkyl (optionally substituted by OH or halo); R 2 = aryl group (optionally substituted) or 1-4C optionally unsaturated (cyclo)alkyl (optionally substituted by halo, OH or heterocycle containing 1-5C and 1-5 heteroatoms selected from O, S or N); X 1 = S, N or O; X 3-X 5 = C or N, provided that no more than two are N; and Y 1 = O or S. Independent claims are also included for: (1) an insecticidal composition (II) comprising (I) together with a support to use (II) as an insecticide; and (2) an insecticidal kit comprising (II) associated with a diffusion means allowing the application of (II) on agricultural, dwelling, forest, marshy, steppe and/or savanna zones. [Image] ACTIVITY : Insecticide; Neuroprotective; Nootropic. MECHANISM OF ACTION : Acetylcholinesterase inhibitor. The ability of (I) to inhibit acetylcholinesterase was tested. The results showed that 5-[(5-methyl-2-furyl)methylene]-1-phenyl-2,4,6(1H,3H,5H)-pyrimidinetrione exhibited IC 50 value of 1.57 mu M and 0.65 mu M against mutated and normal acetylcholinesterases respectively.

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