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  • Title: Synthesis, physicochemical and anticonvulsant properties of new N-4-arylpiperazin-1-yl amides of (2-aza-1,3-dioxospiro[4.4]non-2-yl)- and [4.5]dec-2-yl)-propionic acid.
    Author: Obniska J, Kaminski K, Hondo L, Zejc A.
    Journal: Arch Pharm (Weinheim); 2007 Aug; 340(8):404-8. PubMed ID: 17628031.
    Abstract:
    In continuation of the search of new anticonvulsants, a series of N-4-arylpiperazin-1-yl 2-aza-1,3-dioxospiro[4.4]non-2-yl- (5-8) and [4.5]dec-2-yl- (9-15) propionamides, structurally related to the previously described N-4-arylpiperazin-1-yl amides of 2-aza-1,3-dioxospiro[4.5]dec-2-yl-acetic acid, were synthesized. The designed compounds 5-15 were prepared by condensation of the formerly obtained (2-aza-1,3-dioxospiro[4.5]dec-2-yl)- (3) and (2-aza-1,3-dioxo[4.4]non-2-yl)-(4) propionic acids with the appropriately substituted 4-arylpiperazines, in the presence of the N,N-carbonyldiimidazole (CDIM) reagent. All the compounds were tested for their anticonvulsant activity in the maximum electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) seizure threshold tests. Several compounds 7-10, 13 and 14 revealed protection in the MES screening.
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