Electrophilic natural products and their biological targets
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 …
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 …
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
Quinazolinones, which represent an important part of nitrogen‐containing six‐membered
heterocyclic compounds, are frequently used in drug design due to their wide biological …
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
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 …
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
The peripheral anionic site on acetylcholinesterase (AChE), located at the active center
gorge entry, encompasses overlapping binding sites for allosteric activators and inhibitors; …
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 …
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 …
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 …
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 …
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 …
special attention paid to the fluctuation in the width of the gorge and opening events of the …