Asymmetric synthesis and biological evaluation of hydantoins and derivatives

Abstract

The chemical structure/pharmacological activity study of a compound is of vital importance for the development of new drugs. In this context, N-heterocyclic compounds e.g., hydantoins, become increasingly appreciated mainly due to their anticonvulsant activity, fungicide, herbicide, anti-inflammatory, anti-HIV drugs, analgesic, anti-arritimic, antihypertensive and anti-diabetic. The enzymatic activity of coumarins against the enzyme Acetylcholinesterase (AChE), which is responsible for the neurodegenerative disorders such as Alzheimer´s disease, has been already reported for the heterocyclic compounds. The main objective of this work is the asymmetric synthesis of hydantoins and their derivatives, also the synthesis of hybrid molecules by the introduction of hydantoin ring in the coumarin. The hydantoins synthesis will be performed by reactions between polyisocyanates and aminoacid derivatives, with subsequent cyclization under microwave irradiation, whereas the hybrid compounds will be synthesized by alkylation of coumarins in basic medium in the presence of halides hydantoins. The synthesized compounds will be planned to test against acetylcholinesterase inhibitory activity using a device of liquid chromatography-mass spectrometry (LC-MS). (AU)