engleski

Naphthoxazoles and heterobenzoxazoles: cholinesterase inhibiting and antioxidant activity

Finding novel cholinesterase inhibitors that would be able to cross the blood brain barrier, have favourable pharmacokinetic parameters and reduce hepatotoxicity along with other side- effects, has been the main focus of investigations dealing with Alzheimer’s disease. In this study we evaluated cholinesterase inhibitory and antioxidant activity of seven oxazole derivatives. These compounds have been efficiently and sustainably prepared by photochemical electrocyclization reaction. Various naphthoxazoles have been previously investigated as potential antibacterial, antituberculosis, and anticancer agents. They have also been tested for antioxidant activity, but never for cholinesterase inhibitory activity. Among the tested oxazole derivatives, fused heterobenzoxazole compounds with the pyridine and tiophene moiety, oxazolo[5, 4- h]isoquinoline, thieno[2', 3':5, 6]benzo[1, 2- d]oxazole and thieno[3', 2':5, 6]benzo[1, 2- d]oxazole showed the greatest potential for both the cholinesterase inhibitory and antioxidant activity. Among them the thieno[2', 3':5, 6]benzo[1, 2-d]oxazole was found to be the best one.

antioxidant activity ; cholinesterase activity ; naphthoxazoles ; fused heterobenzoxazoles

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