A series of novel isatin-linked 4,4-dimethyl-5-methylene-4,5-dihydrothiazole-2-thiols (IT2Ts) 1a–1g were designed as acetylcholinesterase (AChE) inhibitors capable interacting with both the catalytic active site (CAS) and peripheral anionic (PAS) enzyme simultaneously. The target IT2Ts prepared through a short synthesis in moderate yield. most potent this 1b 1c (IC50 = 18.2 27.5 μM, respectivel...

New N-allyl/propargyl 4-substituted 1,2,3,4-tetrahydroquinolines derivatives were efficiently synthesized using acid-catalyzed three components cationic imino Diels-Alder reaction (70-95%). All compounds were tested in vitro as dual acetylcholinesterase and butyryl-cholinesterase inhibitors and their potential binding modes, and affinity, were predicted by molecular docking and binding free ene...

Acetylcholinesterase (AChE) inhibition is important because of its health-related implications. Three porphyrin derivatives, Tetraphenylporphinesulfonate (TPPS), 5, 10, 15, 20-Tetrakis (4sulfonatophenyl) porphyrinato Iron (III) Chloride (FeTPPS) and 5, 10, 15, 20-Tetrakis (4-sulfonatophenyl) porphyrinato Iron (III) nitrosyl Chloride (FeNOTPPS), were tested by Molecular Docking as inhibitors of ...

INTRODUCTION A treatment to the Alzheimer's disease consists inhibition of the acetylcholinesterase, which is responsible for the acetylcholine control in the synapses. METHODS We have investigated the potential of inhibition of the acetylcholinesterase produced by hexane extracts of leaves, branches, and flowers from three Bauhinia specimens, which is based on the technique of thin layer chr...

A bis-(-)-nor-meptazinol derivative in which the two meptazinol rings are linked by a nonamethylene spacer is a novel acetylcholinesterase inhibitor that inhibits both catalytic activity and Abeta peptide aggregation. The crystal structure of its complex with Torpedo californica acetylcholinesterase was determined to 2.7 A resolution. The ligand spans the active-site gorge, with one nor-meptazi...

Alternative storage pest control that is more environmentally friendly than the use of synthetic chemical pesticides to botanical from plant essential oils, including clove (Syzygium aromaticum) which contains main compounds eugenol and trans-caryophyllene. To study various mechanisms action oils as insecticides could in silico approach through molecular docking. This aims predict dominant bind...

acetylcholine (ACh) in prefrontal cortex (mPFC) plays an important role in some domains of cognitive function such as attention (1,2), and sensory gating (3). Therefore, measurement of ACh in a living animal is important for the development of novel drugs, as well as investigation of brain function. Microdialysis has proven to be a useful sampling technique in the brain of awake freelymoving an...