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Abstract

Synthesis And CNS Depressant Of Newer Spirobarbiturates

Author(s): B Goel, S Sharma, K Bajaj, D Bansal, T Singh, N Malik, S Lata, C Tyagi, H Panwar, A Agarwal, A Kumar

In an effort to search for more active CNS depressants, a series of spirobarbiturates incorporated with thiazolidinones and azetidinones were synthesized and evaluated for their sedative, hypnotic and anticonvulsant activities. Starting bis compounds (1a-d) were prepared from the reaction of acetone and substituted aldehydes. These bis compounds on Michael addition with barbituric acid give rises to triones (2a-d), which on condensation with NH2NH2.H2O afforded (3a-d) which on reaction with different aromatic aldehydes afforded and Schiff bases (4a-n). These on cyclocondensation with thiolactic acid and chloroacetyl chloride furnished the final products (5a-n) and (6a-n), respectively. Result of toxicity studies and central nervous system depressant activities of these compounds are reported. The structures of the products have been delineated by chemical reaction, elemental analysis and spectral studies.