4.5 Article

Synthesis and molecular docking simulation of new benzimidazole-thiazole hybrids as cholinesterase inhibitors

相关参考文献

注意:仅列出部分参考文献,下载原文获取全部文献信息。
Article Chemistry, Physical

Design, synthesis and molecular docking simulation of oxindole-based derivatives with dual VEGFR-2 and cholinesterase inhibitory activities

Aladdin M. Srour et al.

Summary: Oxindole-based compounds with significant VEGFR-2 and cholinesterase inhibitory properties were synthesized. The best compounds among the tested series displayed inhibitory properties against breast cancer and VEGFR-2 kinase, and some exhibited dual-targeted inhibitory properties against AChE and BChE. Molecular docking studies confirmed the improvement of binding features through substituent variation. These findings suggest the potential of these compounds as lead compounds for dual anti-breast cancer agents and cholinesterase inhibitors.

JOURNAL OF MOLECULAR STRUCTURE (2023)

Article Biochemistry & Molecular Biology

Multipotent Cholinesterase Inhibitors for the Treatment of Alzheimer's Disease: Synthesis, Biological Analysis and Molecular Docking Study of Benzimidazole-Based Thiazole Derivatives

Rafaqat Hussain et al.

Summary: Twenty-four analogues of benzimidazole-based thiazoles were synthesized and evaluated for their inhibitory potential against acetylcholinesterase and butyrylcholinesterase. Molecular docking studies supported the experimental data and provided insights into the interaction between the most active derivatives and amino acids in the enzyme's active site. These findings contribute to understanding the structure-activity relationship and the potential of these compounds as enzyme inhibitors.

MOLECULES (2022)

Article Biochemistry & Molecular Biology

Investigation of the toxicological and inhibitory effects of some benzimidazole agents on acetylcholinesterase and butyrylcholinesterase enzymes

Fikret Turkan

Summary: The study investigated the inhibitory effects of benzimidazole drugs on AChE and BChE enzymes, showing that these compounds can inhibit both enzymes at the nanomolar level in a non-competitive manner. The compound with the highest inhibition of AChE was ricobendazole, while thiabendazole was the most effective in inhibiting BChE. The IC50 and K-i values were calculated for each drug, providing insights into the mechanisms of inhibition.

ARCHIVES OF PHYSIOLOGY AND BIOCHEMISTRY (2021)

Article Biochemistry & Molecular Biology

Structural Modification, In Vitro, In Vivo, Ex Vivo, and In Silico Exploration of Pyrimidine and Pyrrolidine Cores for Targeting Enzymes Associated with Neuroinflammation and Cholinergic Deficit in Alzheimer's Disease

Muhammad Aamir Javed et al.

Summary: A series of derivatives containing pyrimidine and pyrrolidine cores were synthesized and evaluated for their inhibitory activity against COX-2, AChE, and BChE. Some compounds demonstrated excellent inhibition against the targets and showed potential therapeutic effects in both in vitro and in vivo experiments.

ACS CHEMICAL NEUROSCIENCE (2021)

Article Chemistry, Medicinal

Design, synthesis, and biological evaluation of diosgenin-indole derivatives as dual-functional agents for the treatment of Alzheimer's disease

Li-Cheng Zhou et al.

Summary: The study developed diosgenin-indole compounds with potential neuroprotective effects against H2O2, 6-OHDA, and Aβ damages. Compound 5b showed promising results with strong binding affinity to Aβ(1-42), favorable BBB permeation, and absorption abilities. In vivo experiments demonstrated that 5b attenuated memory and learning impairments of Aβ-injected mice, suggesting its potential as a dual-functional neuroprotective agent against AD.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

Article Chemistry, Multidisciplinary

Synthesis and Biological Evaluation of Thiazole-Based Derivatives as Potential Acetylcholinesterase Inhibitors

Aya Y. Hemaida et al.

Summary: Nineteen new thiazole-based derivatives were synthesized and compounds 10 and 16 showed potent AChE inhibitory activities, making them potential lead compounds for the development of new and improved AChE inhibitors.

ACS OMEGA (2021)

Review Biochemistry & Molecular Biology

Expanding therapeutic opportunities for neurodegenerative diseases: A perspective on the important role of phenotypic screening

Susanne E. Swalley

BIOORGANIC & MEDICINAL CHEMISTRY (2020)

Article Biochemistry & Molecular Biology

Gallotannins are uncompetitive inhibitors of pancreatic lipase activity

Elena N. Moreno-Cordova et al.

BIOPHYSICAL CHEMISTRY (2020)

Article Biochemistry & Molecular Biology

Synthesis and 2D-QSAR study of dispiropyrrolodinyl-oxindole based alkaloids as cholinesterase inhibitors

Aladdin M. Srour et al.

BIOORGANIC CHEMISTRY (2019)

Article Biochemistry & Molecular Biology

Synthesis and AChE-Inhibitory Activity of New Benzimidazole Derivatives

Ulviye Acar Cevik et al.

MOLECULES (2019)

Article Oncology

Novel Curcumin Inspired Antineoplastic 1-Sulfonyl-4-Piperidones: Design, Synthesis and Molecular Modeling Studies

Nehmedo G. Fawzy et al.

ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY (2019)

Review Chemistry, Medicinal

Recent advances of thiazole hybrids in biological applications

Mehmet Gumus et al.

FUTURE MEDICINAL CHEMISTRY (2019)

Article Chemistry, Organic

Novel thiazole-piperazine derivatives as potential cholinesterase inhibitors

Seref Demirayak et al.

JOURNAL OF HETEROCYCLIC CHEMISTRY (2019)

Article Chemistry, Medicinal

Thiazole-substituted benzoylpiperazine derivatives as acetylcholinesterase inhibitors

Zafer Sahin et al.

DRUG DEVELOPMENT RESEARCH (2018)

Article Biochemistry & Molecular Biology

Synthesis of some new amide-linked bipyrazoles and their evaluation as anti-inflammatory and analgesic agents

Wissam H. Faour et al.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2016)

Article Chemistry, Medicinal

A computational view on the significance of E-ring in binding of (+)-arisugacin A to acetylcholinesterase

Ziyad F. Al-Rashid et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2015)

Review Biochemistry & Molecular Biology

Oxidative stress and mitochondrial dysfunction in Alzheimer's disease

Xinglong Wang et al.

BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE (2014)

Review Biochemistry & Molecular Biology

Inhibitors of Acetylcholinesterase and Butyrylcholinesterase Meet Immunity

Miroslav Pohanka

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2014)

Article Biochemistry & Molecular Biology

Synthesis, biological activity and molecular modeling studies on 1H-benzimidazole derivatives as acetylcholinesterase inhibitors

Ayse Selcen Alpan et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2013)

Article Biochemistry & Molecular Biology

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

Gulhan Turan-Zitouni et al.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2013)

Article Biochemistry & Molecular Biology

Increasing small molecule drug developability in sub-optimal chemical space

Timothy J. Ritchie et al.

MEDCHEMCOMM (2013)

Review Medicine, Research & Experimental

Alzheimer's Disease: Critical Notes on the History of a Medical Concept

Jesus Ramirez-Bermudez

ARCHIVES OF MEDICAL RESEARCH (2012)

Article Biochemistry & Molecular Biology

Novel coumarin derivatives bearing N-benzyl pyridinium moiety: Potent and dual binding site acetylcholinesterase inhibitors

Masoumeh Alipour et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2012)

Article Clinical Neurology

Biochemical Differentiation of Cholinesterases from Normal and Alzheimer's Disease Cortex

Alexis Ciro et al.

CURRENT ALZHEIMER RESEARCH (2012)

Article Chemistry, Medicinal

Structures of Human Acetylcholinesterase in Complex with Pharmacologically Important Ligands

Jonah Cheung et al.

JOURNAL OF MEDICINAL CHEMISTRY (2012)

Review Behavioral Sciences

Revisiting the cholinergic in the development of Alzheimer's disease

Laura A. Craig et al.

NEUROSCIENCE AND BIOBEHAVIORAL REVIEWS (2011)

Review Clinical Neurology

Oxidative Stress Signaling in Alzheimer's Disease

B. Su et al.

CURRENT ALZHEIMER RESEARCH (2008)

Article Biochemistry & Molecular Biology

Crystal structure of human butyrylcholinesterase and of its complexes with substrate and products

Y Nicolet et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2003)