Design, synthesis and in vivo anticonvulsant screening in mice of novel phenylacetamides

European Journal of Medicinal Chemistry
A V ShindikarC L Viswanathan

Abstract

A set of seven novel N-substituted 2-anilinophenylacetamides were designed by pharmacophore generation and using flexible alignment module of MOE software. The novel molecules were synthesized and screened for anticonvulsant activity in Swiss albino mice by MES and ScPTZ induced seizure tests. Test compounds were found to be potent in MES test. Compounds 12 and 14 were found to be more potent with ED(50) values 24.0 and 8.0 mg kg(-1), respectively, and their activity was comparable to standard drugs (Phenytoin, Carbamazepine). Test compounds did not show significant activity in ScPTZ test. Compounds 12 and 14 also exhibited higher protective indices (20.3 and 87.5, respectively) when assessed for neurotoxicity by rotarod test as compared to the standards.

References

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Citations

Jan 1, 2009·Acta Crystallographica. Section E, Structure Reports Online·Sun Jie, Shuai Shao
Jan 1, 2009·Acta Crystallographica. Section E, Structure Reports Online·Shuai Shao, Jie Sun
Jul 28, 2015·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Maryam BashirBashir Ahmad Chaudhary
Jan 8, 2015·Seizure : the Journal of the British Epilepsy Association·Eunice S M Yuen, Iñaki F Trocóniz
Sep 29, 2011·Archiv der Pharmazie·Anna Pratima G NikaljeAmol Girbane
Jan 9, 2015·Acta Crystallographica. Section C, Structural Chemistry·Lei WangQi Fang
May 14, 2011·The Journal of Organic Chemistry·Donald C Rogness, Richard C Larock

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