Synthesis, molecular docking, antioxidant and cholinestrase inhibitory activity of coumarin based tri-hybridized molecules: An MTDL approach for the development of anti- Alzheimer drugs

Alzheimer’s disease (AD) is one of the most common and prevalent forms of neurodegenerative diseases. Coumarin is a versatile scaffold that exhibits a wide range of biological properties including cholinesterase inhibitory activity and therefore is an important heterocyclic moiety to develop anti-AD drugs. This study focus to design and synthesize coumarin linked 1, 3, 4-oxadiazole hybrid derivatives as multi-target directed ligands (MTDLs). The aim of this project is to design and synthesize novel compounds with multitarget activity for Cholinesterases, COX inhibition with antioxidant activity.

Major Objectives:

(i) To synthesize some novel trihybrids MTDLs by incorporating phenolic acid and oxadiazole in coumarin scaffold (ii) To characterize newly synthesized  compounds by IR, 1H NMR, 13CNMR and mass spectrophotometric techniques (iii) To evaluate AChE, BuChE, antioxidant and COX enzymes inhibitory effects of synthesized compounds at various concentrations To study the structure activity relationship (SAR) and to perform the molecular docking studies

Research Team:

(i) PI: Dr Shah Alam Khan (ii) Co-PI: Dr Khalid Al Balushi

Co-Investigators: (iii) Bushara Al Sabahi (iv) Majed Abukhader