It has been found that derivatives of benzyl N-piperidin-4-one have similar effect than phenytoin drug as an anticonvulsant for the treatment of epilepsy according to docking simulation studies. This is due to the similar binding mode in these chemicals. In this study, a series of six N-piperidinespirohydantoins derivatives were prepared by Bucherer-Bergs reaction, from corresponding N-piperidin-4-ones derivatives benzyl and phenethyl groups, substituted in the aromatic ring with metoxy and nitro groups. The hydantoins were evaluated for anticonvulsant activity with maximal electroshock (MES) induced method in vivo in male Wistar rats in the treatment of epilepsy.
Virtual Screening of Putative Anticonvulsant Hydantoin Derived Drugs and Biological Evaluation / Santiago Ruiz, Sandy; Polverini, Eugenia; Manjarrez, Joaquin; Espinoza, Karla A.; Reynoso, Edgar; Rivero, Ignacio A.. - In: ANNALS OF MEDICINAL CHEMISTRY AND RESEARCH. - ISSN 2378-9336. - 2:1(2016), pp. 1016-1022.
Virtual Screening of Putative Anticonvulsant Hydantoin Derived Drugs and Biological Evaluation
POLVERINI, Eugenia;
2016-01-01
Abstract
It has been found that derivatives of benzyl N-piperidin-4-one have similar effect than phenytoin drug as an anticonvulsant for the treatment of epilepsy according to docking simulation studies. This is due to the similar binding mode in these chemicals. In this study, a series of six N-piperidinespirohydantoins derivatives were prepared by Bucherer-Bergs reaction, from corresponding N-piperidin-4-ones derivatives benzyl and phenethyl groups, substituted in the aromatic ring with metoxy and nitro groups. The hydantoins were evaluated for anticonvulsant activity with maximal electroshock (MES) induced method in vivo in male Wistar rats in the treatment of epilepsy.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.