Synthesis, biological assessment and molecular modeling of new dihydroquinoline-3-carboxamides and dihydroquinoline-3-carbohydrazide derivatives as cholinesterase inhibitors, and Ca channel antagonists

Novel Tacrine‐Grafted Ugi Adducts as Multipotent Anti‐Alzheimer Drugs: A Synthetic Renewal in Tacrine–Ferulic Acid Hybrids

“…[26] Therefore, they seem well suited to the search for new molecules with different moieties of interest that are able to interact with various pathological events in connection with AD. [4,[27][28][29] Particularly interesting among these types of reactions is the Ugi four-component reaction (U-4CR). This transformation allows the creation of up to five points of structural diversity in one pot which can be very useful for the expeditious synthesis of bioactive molecules for multifactorial diseases such as AD.…”

“…[ [4][5][6] Two cholinesterases, acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), are responsible for hydrolysis of the neurotransmitter ACh in the brain. Recent evidence has highlighted a non-classical role for cholinergic enzymes, which may be important for the development of more effective drugs for AD.…”

Synthesis and pharmacological evaluation of donepezil-based agents as new cholinesterase/monoamine oxidase inhibitors for the potential application against Alzheimer’s disease

“…Based on the results of ChEs and MAOs inhibitory activity, compounds w10, 11,14,15,18,21,22 showed good inhibition. However, their ChE inhibitory activity was initially tested on enzymes of animal origin due to the lower cost.…”

“…At present, there are three FDA-approved drugs for AD treatment, these anti-AChE agents include galanthamine, donepezil, and rivastigmine, which can only provide a temporary symptom alleviation instead of preventing or slowing the progressive neurodegeneration [21][22][23] . However, the multiple etiologies of AD make single-target strategy difficult to shed good therapeutic effect.…”

Synthesis and biological evaluation of some thiazole derivatives as new cholinesterase inhibitors

“…In a previous work, the inhibition of AChE by thiamine and its derivatives was investigated and structureactivity relationship study was also carried out to identify structural features that are associated with the inhibitory potency of these compounds 16 . Some researchers also carried out considerable research for novel cholinesterase inhibitors bearing amide and hydrazide moieties previously 17 . On the basis of these findings, we became interested in biological evaluation of thiazoles as anticholinesterase agents.…”