A novel catalytic synthesis of 3,3'-(arylmethylene)-bis-(4-hydroxy-2H-chromene-2-one) derivatives from a tandem condensation reaction of 4-hydroxycoumarin and aromatic aldehydes has been developed. The reaction occurs in water in the presence of Melamine trisulfonic acid as catalyst to give the corresponding products in good to high yields. This green approach has several advantages such as sho...

Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) are the key enzymes in pathogenesis of Alzheimer's disease (AD), which is characterized by a deficit in central cholinergic transmission. In the current study, AChE and BChE inhibitory activities of seven coumarin derivatives [umbelliferone (1), 4-methylumbelliferone (2), 4-hydroxycoumarin (3), scopoletin (4), 8-methoxypsoralen (5), b...

C2-symmetric diimine generated in situ from (R,R)-HPEN and 8-formylquinoline was readily transformed to novel chiral pre-III bearing 1(S),2(S)-bis(quinolin-8-yl) ethane salicylic aldehyde fragments via stereoselective diaza-Cope rearrangement. The structure absolute configuration of the product established by X-ray diffraction study corresponding Rh(III) complex. In presence pre-III, practicall...

A series of 7-hydroxycoumarin derivatives connected by an amidic linker to the different amines were designed and synthesized as cholinesterase inhibitors. Most compounds showed remarkable inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Among them, N-(1-benzylpiperidin-4-yl)acetamide derivative 4r with IC50 value of 1.6 μM was the most potent compound ...

Difenacoum is a new rodenticide recently introduced on the British market; it is one of the most potent of a series of hydroxycoumarin-based anticoagulants. Difenacoum is effective against laboratory rats and mice resistant to conventional anticoagulants and has a marked selectivity in favour of non-target species. Vitamin K1 is an effective antidote and the hazard of secondary poisoning is min...