New Benzamides as Multi-Targeted Compounds: A Study on Synthesis, AChE and BACE1 Inhibitory Activity and Molecular Docking

New Benzamides as Multi-Targeted Compounds: A Study on Synthesis, AChE and BACE1 Inhibitory Activity and Molecular Docking

The synthesis of eleven new and previously undescribed benzamides was designed. These compounds were specifically projected as potential inhibitors of the enzymes acetylcholinesterase (AChE) and β-secretase (BACE1). N,N′-(1,4-phenylene)bis(3-methoxybenzamide) was most active against AChE, with an in...

Full description

Bibliographic Details
Main Authors:	Danuta Drozdowska, Dawid Maliszewski, Agnieszka Wróbel, Artur Ratkiewicz, Michał Sienkiewicz
Format:	Article
Language:	English
Published:	MDPI AG 2023-10-01
Series:	International Journal of Molecular Sciences
Subjects:	Alzheimer’s disease AChE inhibitors BACE1 inhibitors benzamides dual inhibitors
Online Access:	https://www.mdpi.com/1422-0067/24/19/14901

Similar Items

Development of Activity Rules and Chemical Fragment Design for In Silico Discovery of AChE and BACE1 Dual Inhibitors against Alzheimer’s Disease
by: Le-Quang Bao, et al.
Published: (2023-04-01)

Dual Inhibitors of AChE and BACE-1 for Reducing Aβ in Alzheimer’s Disease: From In Silico to In Vivo
by: Noa Stern, et al.
Published: (2022-10-01)

Perspectives for New and More Efficient Multifunctional Ligands for Alzheimer′s Disease Therapy
by: Agnieszka Zagórska, et al.
Published: (2020-07-01)

Development and Structural Modification of BACE1 Inhibitors
by: Ting Gu, et al.
Published: (2016-12-01)

Discovery of Indole-Containing Benzamide Derivatives as HDAC1 Inhibitors with In Vitro and In Vivo Antitumor Activities
by: Xiu Gu, et al.
Published: (2022-06-01)

Synthesis, In Silico and In Vitro Evaluation for Acetylcholinesterase and BACE-1 Inhibitory Activity of Some <i>N</i>-Substituted-4-Phenothiazine-Chalcones
by: Thai-Son Tran, et al.
Published: (2020-08-01)

Design, in silico and pharmacological evaluation of a peptide inhibitor of BACE-1
by: Renata Boldin, et al.
Published: (2023-06-01)

Structure–activity relationship investigation of benzamide and picolinamide derivatives containing dimethylamine side chain as acetylcholinesterase inhibitors
by: Xiao-hui Gao, et al.
Published: (2018-01-01)

Design, synthesis and biological evaluation of 4-bromo-N-(3,5-dimethoxyphenyl)benzamide derivatives as novel FGFR1 inhibitors for treatment of non-small cell lung cancer
by: Zixin Xie, et al.
Published: (2018-01-01)

Patterned Superhydrophobic SERS Substrates for Sample Pre-Concentration and Demonstration of Its Utility through Monitoring of Inhibitory Effects of Paraoxon and Carbaryl on AChE
by: Umi Yamaguchi, et al.
Published: (2020-05-01)

Latest advances in dual inhibitors of acetylcholinesterase and monoamine oxidase B against Alzheimer’s disease
by: Dajiang Zou, et al.
Published: (2023-12-01)

Synthesis of novel substituted N-aryl benzamides as hA3G stabilizers and their inhibitory activities against hepatitis C virus replication
by: Yanping Li, et al.
Published: (2013-09-01)

Multitarget drugs as potential therapeutic agents for alzheimer’s disease. A new family of 5-substituted indazole derivatives as cholinergic and BACE1 inhibitors
by: Pedro González-Naranjo, et al.
Published: (2022-12-01)

Discovery of benzamide-hydroxypyridinone hybrids as potent multi-targeting agents for the treatment of Alzheimer's disease
by: Xiaoying Jiang, et al.
Published: (2021-01-01)

The BACE‐1 inhibitor CNP520 for prevention trials in Alzheimer's disease
by: Ulf Neumann, et al.
Published: (2018-11-01)

New Highly Selective BACE1 Inhibitors and Their Effects on Dendritic Spine Density In Vivo
by: Katrin Pratsch, et al.
Published: (2023-07-01)

Extensive Structure Modification on Luteolin-Cinnamic Acid Conjugates Leading to BACE1 Inhibitors with Optimal Pharmacological Properties
by: De-Yang Sun, et al.
Published: (2019-12-01)

One Pot Synthesis of Micromolar BACE-1 Inhibitors Based on the Dihydropyrimidinone Scaffold and Their Thia and Imino Analogues
by: Jessica Bais, et al.
Published: (2020-09-01)

Design, synthesis, molecular modeling and biological evaluation of novel Benzoxazole-Benzamide conjugates via a 2-Thioacetamido linker as potential anti-proliferative agents, VEGFR-2 inhibitors and apoptotic inducers
by: Ibrahim H. Eissa, et al.
Published: (2022-12-01)

Synthesis, Biological Activity, and Molecular Dynamics Study of Novel Series of a Trimethoprim Analogs as Multi-Targeted Compounds: Dihydrofolate Reductase (DHFR) Inhibitors and DNA-Binding Agents
by: Agnieszka Wróbel, et al.
Published: (2021-04-01)

From BACE1 Inhibitor to Multifunctionality of Tryptoline and Tryptamine Triazole Derivatives for Alzheimer’s Disease
by: Jutamas Jiaranaikulwanitch, et al.
Published: (2012-07-01)

Synthesis, Biological Activities and Docking Studies of Novel 4-(Arylaminomethyl)benzamide Derivatives as Potential Tyrosine Kinase Inhibitors
by: Elena Kalinichenko, et al.
Published: (2019-09-01)

1,3,5-Triazine Nitrogen Mustards with Different Peptide Group as Innovative Candidates for AChE and BACE1 Inhibitors
by: Dawid Maliszewski, et al.
Published: (2021-06-01)

Prediction of Drug Potencies of BACE1 Inhibitors: A Molecular Dynamics Simulation and MM_GB(PB)SA Scoring
by: Mazen Y. Hamed
Published: (2020-12-01)

Novel acetylcholinesterase inhibitors: Synthesis, docking and inhibitory activity evaluation of 4-benzamido-N-(1-benzylpiperidin-4-yl) benzamide derivatives
by: Ahmad Mohammadi-Farani, et al.
Published: (2024-01-01)

Passive immunotherapy with a novel antibody against 3pE-modified Aβ demonstrates potential for enhanced efficacy and favorable safety in combination with BACE inhibitor treatment in plaque-depositing mice
by: Jonathan Janssens, et al.
Published: (2021-07-01)

Crystal structure of 2-fluoro-N-(1,3-thiazol-2-yl)benzamide
by: Rodolfo Moreno-Fuquen, et al.
Published: (2015-11-01)

Navigating the GSK-3β inhibitors as versatile multi-target drug ligands in Alzheimer’s disease intervention – A comprehensive review
by: Nachiket Jitendra Joshi, et al.
Published: (2024-01-01)

Highlights in BACE1 Inhibitors for Alzheimer's Disease Treatment
by: Judite R. M. Coimbra, et al.
Published: (2018-05-01)

Allostery Inhibition of BACE1 by Psychotic and Meroterpenoid Drugs in Alzheimer’s Disease Therapy
by: Samuel C. Ugbaja, et al.
Published: (2022-07-01)

Identification of new allosteric sites and modulators of AChE through computational and experimental tools
by: Carlos Roca, et al.
Published: (2018-01-01)

Pharmacodynamics of atabecestat (JNJ-54861911), an oral BACE1 inhibitor in patients with early Alzheimer’s disease: randomized, double-blind, placebo-controlled study
by: Maarten Timmers, et al.
Published: (2018-08-01)

Discovery of novel isoflavone derivatives as AChE/BuChE dual-targeted inhibitors: synthesis, biological evaluation and molecular modelling
by: Bo Feng, et al.
Published: (2017-01-01)

DL0410 Ameliorates Memory and Cognitive Impairments Induced by Scopolamine via Increasing Cholinergic Neurotransmission in Mice
by: Wenwen Lian, et al.
Published: (2017-03-01)

HDAC Inhibitors for the Therapy of Triple Negative Breast Cancer
by: Cristina Maccallini, et al.
Published: (2022-05-01)

In Silico Docking and In Vitro Approaches towards BACE1 and Cholinesterases Inhibitory Effect of Citrus Flavanones
by: Seungeun Lee, et al.
Published: (2018-06-01)

Accelerated long‐term forgetting is a BACE1 inhibitor‐reversible incipient cognitive phenotype in Alzheimer’s disease model mice
by: Masuo Ohno
Published: (2021-06-01)

FOXA1 Regulation Turns Benzamide HDACi Treatment Effect-Specific in BC, Promoting NIS Gene-Mediated Targeted Radioiodine Therapy
by: Maitreyi Rathod, et al.
Published: (2020-12-01)

Chromeno[3,4-<i>b</i>]xanthones as First-in-Class AChE and Aβ Aggregation Dual-Inhibitors
by: Daniela Malafaia, et al.
Published: (2021-04-01)

Two New AChE Inhibitors Isolated from Li Folk Herb Heilaohu “<i>Kadsura coccinea</i>” Stems
by: Sheng Zhuo Huang, et al.
Published: (2019-10-01)