Electrophilic natural products and their biological targets

M Gersch, J Kreuzer, SA Sieber - Natural product reports, 2012 - pubs.rsc.org
Covering: 1900 to 2011 The study of biologically active natural products has resulted in
seminal contributions to our understanding of living systems. In the case of electrophilic …

[PDF][PDF] Peripheral and dual binding site acetylcholinesterase inhibitors: implications in treatment of Alzheimer's disease

A Castro, A Martinez - Mini reviews in medicinal chemistry, 2001 - researchgate.net
Recently advances in understanding the molecular basis of Alzheimer's disease have led to
the consideration of the relationship between cholinergic inhibitors and amyloid deposition …

Novel Quinazolinone Derivatives: Potential Synthetic Analogs for the Treatment of Glaucoma, Alzheimer's Disease and Diabetes Mellitus

FS Tokalı, P Taslimi, B Tuzun, A Karakuş… - Chemistry & …, 2023 - Wiley Online Library
Quinazolinones, which represent an important part of nitrogen‐containing six‐membered
heterocyclic compounds, are frequently used in drug design due to their wide biological …

Synthesis of new carboxylates and sulfonates containing thiazolidin-4-one ring and evaluation of inhibitory properties against some metabolic enzymes

FS Tokalı, P Taslimi, B Tüzün, A Karakuş… - Journal of the Iranian …, 2023 - Springer
A series of thizaolidin-4-one derivatives (3a-o) was synthesized with excellent yield (94–
97%) and the structures of the compounds were characterized with Fourier-transform …

[HTML][HTML] Structural insights into ligand interactions at the acetylcholinesterase peripheral anionic site

Y Bourne, P Taylor, Z Radić, P Marchot - The EMBO journal, 2003 - embopress.org
The peripheral anionic site on acetylcholinesterase (AChE), located at the active center
gorge entry, encompasses overlapping binding sites for allosteric activators and inhibitors; …

Kinetic and Structural Studies on the Interaction of Cholinesterases with the Anti-Alzheimer Drug Rivastigmine,

P Bar-On, CB Millard, M Harel, H Dvir, A Enz… - Biochemistry, 2002 - ACS Publications
Rivastigmine, a carbamate inhibitor of acetylcholinesterase, is already in use for treatment of
Alzheimer's disease under the trade name of Exelon. Rivastigmine carbamylates Torpedo …

Donepezil–tacrine hybrid related derivatives as new dual binding site inhibitors of AChE

D Alonso, I Dorronsoro, L Rubio, P Munoz… - Bioorganic & medicinal …, 2005 - Elsevier
A new series of donepezil–tacrine hybrid related derivatives have been synthesised as dual
acetylcholinesterase inhibitors that could bind simultaneously to the peripheral and catalytic …

Three‐dimensional structure of a complex of galanthamine (Nivalin®) with acetylcholinesterase from Torpedo californica: Implications for the design of new anti …

C Bartolucci, E Perola, C Pilger, G Fels… - Proteins: structure …, 2001 - Wiley Online Library
The 3D structure of a complex of the anti‐Alzheimer drug galanthamine with Torpedo
californica acetylcholinesterase is reported. Galanthamine, a tertiary alkaloid extracted from …

[HTML][HTML] Crystal structure of human carboxylesterase 1 complexed with the Alzheimer's drug tacrine: from binding promiscuity to selective inhibition

S Bencharit, CL Morton, JL Hyatt, P Kuhn, MK Danks… - Chemistry & biology, 2003 - cell.com
Abstract Human carboxylesterase 1 (hCE1) is a broad-spectrum bioscavenger that plays
important roles in narcotic metabolism, clinical prodrug activation, and the processing of fatty …

[HTML][HTML] Analysis of a 10-ns molecular dynamics simulation of mouse acetylcholinesterase

K Tai, T Shen, U Börjesson, M Philippopoulos… - Biophysical journal, 2001 - cell.com
A 10-ns molecular dynamics simulation of mouse acetylcholinesterase was analyzed, with
special attention paid to the fluctuation in the width of the gorge and opening events of the …