Anticonvulsant and Neurotoxicity Evaluation of Some Newly Synthesized Thiazolyl Coumarin Derivatives

Abstract

The present series of compounds were synthesized with the aim to develop newer anticonvulsant agents that are comparatively more efficacious and safer than the currently used anticonvulsant agents. Various thiazolyl coumarins were synthesized by the reaction of 3-(bromoacetyl)-2H-chromen-2-one with different substituted aryl thiourea. The structures of the synthesized compounds were confirmed by spectral data and elemental analyses. Compounds were tested for anticonvulsant activity utilizing Pen Tylenetetra Zoleinduced seizure (PTZ) and Maximal Electroshock Seizure (MES) tests at 30, 100 and 300 mg kg −1 dose level. Neurotoxicity and ethanol potentiation test of the compounds were also assessed at the same dose level. Two compounds of the series 3g and 3j exhibited significant anticonvulsant activity at 30 mg kg −1 dose level with lesser neurotoxicity than the standard drug phenytoin.

Synthetic and natural coumarins as potent anticonvulsant agents: A review with structure–activity relationship

“…Also, author reported the sizes of the group also played an important role as the derivatives substituted with -fluoro group were most active followed by -chloro and -nitro. 77 Batra et al studied a series coumarin-carbohydrazides and their corresponding thiazolidinone derivatives on the basis of pharmacophoric distance mapping study and evaluated for neurotoxicity by rotorod test, anticonvulsant activity by MES animal model of seizures. Compounds (28) and (29) showed considerable protection against seizures and considered as the prototype molecules of the series, and their ED 50 values were found to be lesser than 150 μmol/ kg.…”

Synthesis and anti-acetylcholinesterase activities of novel glycosyl coumarylthiazole derivatives

“…Coumarin-thiazole compounds have many activities such as antibacterial, antioxidant, anticonvulsive, anticancer, and for treating hypertension. [17][18][19][20][21] Combining multiple active molecules within the same structure is an important means to synthesize new substances, and it is also the main way to find compounds with new biological and physiological activities. Based on the above analysis, we have designed and synthesized a series of novel glycosyl coumarylthiazole derivatives in order to find new and effective AChE inhibitors.…”

“…Coumarinthiazole compounds have many activities such as antibacterial, antioxidant, anticonvulsive, anticancer, and for treating hypertension. [17][18][19][20][21] Combining multiple active molecules…”

Design, Synthesis, Anti-inflammatory & Anticonvulsant Activity of Substituted Heterocyclic Compounds

“…But these drugs may cause side effects like skin rashes, poor coordination, tiredness, fatigue, dizziness, short memory, confusion etc [20]. These undesirable side effects necessities need of development of new anticonvulsant derivatives [21]. After review of literature, Coumarin has shown potential in different biological activities and can open new arena for the development of new substituted derivatives.…”