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

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.

[
  "009:25"
]

[
  "009:066"
]

[
  "NIH"
]