J. R. Patel, B. Dholakiya, Nibha Mishra
Apr 1, 2013
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Influential Citations
3
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Quality indicators
Journal
Journal of Pharmacy Research
Abstract
Abstract Background Preparation of a new series of Michael adducts as an 1-(4-acetylphenyl)-3-aryloxypyrrolidine-2,5-dione derivates using cellulose sulfuric acid catalyst with objective of obtaining lead compounds for future development as anticonvulsants. Methods The inhibition by economically and efficiently synthesized targeted 1-(4-acetylphenyl)-3-aryloxypyrrolidine-2,5-diones 5a–n with γ-aminobutyric acid (GABA)-transaminase activity was studied with homogenized mice brain as described by Fowler & Qume followed by the fluorimetric analysis using Salvador & Albers method. All the compounds were characterized by physical, spectroscopic and elemental analysis. Results and discussion Among the fourteen Michael adducts of 1-(4-acetylphenyl)-pyrrole-2,5-dione, 1-(4-acetylphenyl)-3-(4-Bromophenyloxy)-pyrrolidine-2,5-dione 5d and 1-(4-acetylphenyl)-3-(Salicyldehydoxy)-pyrrolidine-2,5-dione 5h showed more potent as in vitro barain GABA-transaminase activity with IC 50 (100.5 ± 5.2 μM) and IC 50 (160.4 ± 6.2 μM) respectively. This activity study was performed by using the fluorimetric analytical evaluation data compared with vigabatrin, a reference standard drug. Conclusion In conclusion, 1-(4-acetylphenyl)-3-(4-Bromophenyloxy)-pyrrolidine-2,5-dione 5d and 1-(4-acetylphenyl)-3-(Salicyldehydoxy)-pyrrolidine-2,5-dione 5h strongly fulfill where as 1-(4-acetylphenyl)-3-(2,4,6-Nitrophenyloxy)-pyrrolidine-2,5-dione 5l and 1-(4-acetylphenyl)-3-(2-Napthyloxy)-pyrrolidine-2,5-dione 5b significantly fulfill the criteria for mice brain GABA-T inhibitory agents.