Synthesis, physicochemical and anticonvulsant properties of N-benzyl and N-aminophenyl derivatives of 2-azaspiro[4.4]nonane and [4.5]decane-1,3-dione. Part I

Add time:09/30/2019    Source:infona.pl

To continue our systematic SAR studies, two series of N-benzyl- (X=CH 2 ) and N-aminophenyl- (X=NH) derivatives of 2-AZASPIRO[4.4]NONANE (cas 175-94-0) (1a–1j) and 2-azaspiro[4.5]decane-1,3-dione (2a–2j) were synthesized, and evaluated in maximum electroshock seizure (MES), subcutaneous pentylenetetrazole (sc.MET) and rotorod (TOX) tests for their anticonvulsant activity. Among those derivatives, the most potent N-aminophenyl-2-azaspiro[4.4]nonane-1,3-dione 1j had ED 50 = 76.27 mg kg –1 . X-ray structures for two pairs of derivatives with a different linker were solved. Then 3-D data for the active 1j versus less active 2j, both having an imine linker (X=NH), and the respective parent of compounds with a methylene linker (X=CH 2 ) (1a and 2a) were discussed.

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