Abstract
We report here the synthesis and in vivo anticonvulsant/neurotoxicity activities of a series of compounds belonging to 2-aryl-4-arylidene-1-phenyl-1H-imidazol-5(4H)-one. The scaffold is based on the commonality of 5-membered lactam ring structures as successful anticonvulsant agents. The present compounds exhibited a range of anticonvulsant activity in pentylenetetrazole (PTZ)-induced seizure test. In particular, the protection was excellent by compounds bearing furylmethylidene on C4, possibly due to good pharmacokinetic properties. It was found that high lipophilicity and/or electron deficient aryl ring substitution at C4 compromised the anticonvulsant activities. For example, chloro analogues were found much less active than unsubstituted phenyl or furyl derivatives. Regarding side effects, active compounds exerted no observable neurotoxic effect at their therapeutic doses in Chimney test.
Highlights
Interest in developing new anticonvulsant medicines is still high after a century of introducing phenobarbital in 1912 [1]
We report here the synthesis and in vivo anticonvulsant/neurotoxicity activities of a series of compounds belonging to 2-aryl-4-arylidene-1-phenyl-1H-imidazol-5(4H)-one
The present compounds exhibited a range of anticonvulsant activity in pentylenetetrazole (PTZ)-induced seizure test
Summary
Interest in developing new anticonvulsant medicines is still high after a century of introducing phenobarbital in 1912 [1]. The estimated proportion of the general population with active epilepsy at a given time is between 4 and 10 per 1000 people [3] This ratio is doubled in developing countries as they harbor more than 90% of active epileptic cases. Regardless the fact that there are at least 20 FDA approved antiepileptic drugs (Examples, Figure 1(a)) [5], the control of epileptic seizures stays around 70% of active epileptic cases only [6]. This underscores the need for continuing the research aiming at developing new antiepileptic agents to help patients not responding to current medicines [7]. We decided to investigate the potentiality of imidazolone derivatives as anticonvulsants against their neurotoxic side effects
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