Synthesis and Evaluation of Anticonvulsant Activity of Some 5,5-Disubstituted-N3-[(2-aryl thiazolidine-4-one-3-yl)amino]hydantoins

Abstract

According to the World Health Organization, the majority of people with epilepsy who live in developing countries do not have access to high-quality treatment. Modern anticonvulsants are in high demand since the unwanted effects of those compounds already in use make therapy difficult. The synthesis of derivatives of 5,5-disubstituted-N3-[(2-aryl thiazolidine-4-one-3-yl)amino]hydantoins has been reported. The position N3 of the hydantoin nucleus was substituted with 4-thiazolidinone moiety containing aryl substituent at 2nd position with the goal of achieving the enhanced anticonvulsant effect. Compounds 5c, 5d, 5l, 5r showed significant activity among the evaluated compounds compared to control at dose of 45 mg/kg. The analysis of structural features revealed that the substitution of p-hydroxy phenyl and cinnamyl substituted at 2nd position of thiazolidinone ring in 5,5-diphenyl-2,4- imidazolidinedione and p-chloro phenyl, p-methoxy phenyl substituted at 2nd position of thiazolidinone ring in (5,5-dialkyl)/(5-alkyl-5-substitutedphenyl)-2,4-imidazolidinedione skeleton enhanced the anticonvulsant potentiality of the synthesized compounds.

Synthesis, <i>In-vivo</i> estimation of Novel 3-(6-Substituted Benzthiazole-2-yl /Oxadiazole-2-yl)-2-Substituted 4-Quinazolineones

“…It is one of the noteworthy heterocycle groupings with diverse biological characteristics. In continuation of our efforts [14][15][16] to develop new antiepileptic compounds, In this work, we propose to synthesize the coupling of quinazolinones conjugated with heterocycles, namely 1,3,4-oxadiazole and Aminobenzthiazole moieties, in order to achieve enhanced anticonvulsant action and generate lead compounds.…”