Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants.

Epilepsy is one of the commonly prevailing neurological disorders. According to the reports, it is evident that about 80% of the epileptic cases have been observed in developing countries. Although there are many drugs with significant potency available in the market; still there is an issue of selectivity and toxicity. Therefore, continuous attempts have been made by the researchers to develop newer therapeutic agents against epilepsy. Many synthetic strategies have been available in the literature to synthesize various classes of anticonvulsants with promising activity. In the presented review, authors have summarized some newer synthetic routes being used for the synthesis of nitrogen-containing anticonvulsants taking a cue from the reported established anticonvulsant drugs viz. vigabatrin, sodium valproate, oxcarbazepine, felbamate, retigabine, and gabapentin. Various derivatives with the substitution for better anticonvulsant profile have been described in the figures for easy comparative study. The structure-activity relationship (SAR) of compounds with maximum potency has also been discussed. This article may serve as a boost for the researchers to modify the pre-existing synthetic routes as well as to improve potency and yield of the compounds.

Neurological and psychiatric management using COMT inhibitors: A review.

The increase in psychiatric and neurological disorders includes Parkinson's, Schizophrenia, Alzheimer's and Depression over the last 50 years adds concerns to society. In contrast, there have been great advances in elucidating the receptors of CNS and their interaction with the novel molecules. Enzymes inhibitors are on the top plan to interact specifically with the targets for better potency and reduce the toxic effects. COMT inhibitors work by inhibiting the conversion of catechols including dopamine to its inactive degradation products. This makes the availability of l-dopa to the brain and thus alleviating the symptoms of CNS disorders. Substitution pattern and the structural requirements for better binding within the receptors are important for the drug findings. Apart from catechol modification, some non-catechol based potent COMT inhibitors are also discussed. A detailed guide regarding inhibition of S-adenosyl-l-methionine, catalyzing the transfer of the methyl group by COMT is also represented. This review discusses the thorough development of COMT inhibitors right from the beginning until the present. The derivatives are discussed along with their structure-activity relationship having structural substitution prerequisites for the development of more potent novel COMT inhibitors.