Synthesis, Biological Evaluation, and In Silico Characterization of Novel Imidazothiadiazole–Chalcone Hybrids as Multi-Target Enzyme Inhibitors

Synthesis, Biological Evaluation, and In Silico Characterization of Novel Imidazothiadiazole–Chalcone Hybrids as Multi-Target Enzyme Inhibitors

<b>Background/Objectives:</b> The need for dual-targeted enzyme inhibitors is critical in addressing complex diseases like Alzheimer’s and glaucoma. Imidazothiadiazole and chalcone moieties are known for diverse bioactivities. This study aimed to develop novel imidazothiadiazole–chalcone...

Full description

Saved in:

Bibliographic Details
Main Authors:	Hakan Alici, Senol Topuz, Kadir Demir, Parham Taslimi, Hakan Tahtaci
Format:	Article
Language:	English
Published:	MDPI AG 2025-06-01
Series:	Pharmaceuticals
Subjects:	imidazothiadiazole chalcone hybrids carbonic anhydrase inhibitors acetylcholinesterase inhibitors butyrylcholinesterase inhibitors molecular docking
Online Access:	https://www.mdpi.com/1424-8247/18/7/962
Tags:	Add Tag No Tags, Be the first to tag this record!

Similar Items

Design and evaluation of substituted cinnamoyl piperidinyl acetate derivatives as potent cholinesterase inhibitors
by: Maryam Esmkhani, et al.
Published: (2025-06-01)

Neuropharmacological Assessment of Sulfonamide Derivatives of Para-Aminobenzoic Acid through In Vivo and In Silico Approaches
by: Ankit Ganeshpurkar, et al.
Published: (2024-10-01)

In Vitro Evaluation of Novel Furo[3,2-<i>c</i>]coumarins as Cholinesterases and Monoamine Oxidases Inhibitors
by: Mariagrazia Rullo, et al.
Published: (2025-04-01)

Synthesis and anti-Alzheimer activity of new N-(5, 6-dimethyl-1H-benzo[d] imidazol-2-yl)-1-phenylmethanimine derivatives
by: Hiba Ali Hasan, et al.
Published: (2024-10-01)

RECENT ADVANCES OF CHOLINESTERASE INHIBITORS PLAYING A CRITICAL ROLE IN THE TREATMENT OF ALZHEIMER’S DISEASE (2020-2022)
by: Elmas Rumeysa Yıldırım, et al.
Published: (2023-06-01)

Comparison of In Silico AChE Inhibitory Potentials of Some Donepezil Analogues
by: Mehmet Koca
Published: (2024-04-01)

Exploring Chalcone Derivatives as a Multifunctional Therapeutic Agent: Investigating Antioxidant Potential, Acetylcholinesterase Inhibition and Computational Insights
by: Sujatha M. Lokanath, et al.
Published: (2025-04-01)

Assessment of Potential Acetylcholinesterase Inhibitors: An In Silico Study
by: Nathaniel Ohiemi Amedu, et al.
Published: (2024-08-01)

Synthesis, carbonic anhydrase inhibition studies and modelling investigations of phthalimide–hydantoin hybrids
by: Morteza Abdoli, et al.
Published: (2024-12-01)

4-Anilinoquinazoline-based benzenesulfonamides as nanomolar inhibitors of carbonic anhydrase isoforms I, II, IX, and XII: design, synthesis, in-vitro, and in-silico biological studies
by: Hossam Nada, et al.
Published: (2022-12-01)

Novel 3-(6-methylpyridin-2-yl)coumarin-based chalcones as selective inhibitors of cancer-related carbonic anhydrases IX and XII endowed with anti-proliferative activity
by: Haytham O. Tawfik, et al.
Published: (2022-12-01)

Ligands affinity for regulatory sites of human acetylcholesterase and butyrylcholinesterase: A comparative bioinformatic analysis
by: A.R. Mukhametgalieva, et al.
Published: (2021-03-01)

A Novel Galantamine–Curcumin Hybrid Inhibits Butyrylcholinesterase: A Molecular Dynamics Study
by: Evdokiya Salamanova, et al.
Published: (2024-12-01)

Anticholinesterase Activity and Bioactive Compound Profiling of Six Hop (<i>Humulus lupulus</i> L.) Varieties
by: Bartłomiej Sagan, et al.
Published: (2024-12-01)

Can Marine Products Improve Alzheimer’s Disease
by: Hamid-Reza Adhami, et al.
Published: (2020-11-01)

Arylsulfonamido-alkyl-sulfamates act as inhibitors of bovine carbonic anhydrase II
by: Toni C. Denner, et al.
Published: (2024-12-01)

A Review of Natural and Synthetic Chalcones as Anticancer Agents Targeting Topoisomerase Enzymes
by: François-Xavier Toublet, et al.
Published: (2025-06-01)

Dyhidro-β-agarofurans natural and synthetic as acetylcholinesterase and COX inhibitors: interaction with the peripheral anionic site (AChE-PAS), and anti-inflammatory potentials
by: Julio Alarcón-Enos, et al.
Published: (2022-12-01)

Etonogestrel and Alzheimer's: A multi-scale computational approach to acetylcholinesterase inhibition
by: Kunal Bhattacharya, et al.
Published: (2025-07-01)

Discovery, Biological Evaluation and Binding Mode Investigation of Novel Butyrylcholinesterase Inhibitors Through Hybrid Virtual Screening
by: Lizi Li, et al.
Published: (2025-05-01)

Prospects for the application of inhibitors of carbonic anhydrase isoforms IX and XII in oncology
by: S. А. Kalinin, et al.
Published: (2024-04-01)

Derivatives of Amodiaquine as Potent Human Cholinesterases Inhibitors: Implication for Treatment of Alzheimer’s Disease
by: Ana Matošević, et al.
Published: (2024-11-01)

In Silico and In Vivo Evaluation of a New Derivative from Memantine and Sinapic Acid (<i>N</i>-Sinapoyl-memantine) as a Candidate for the Management of Alzheimer’s Disease
by: Andrey Popatanasov, et al.
Published: (2025-05-01)

Novel 4-hydroxycoumarin Derivatives Linked to N-benzyl Pyridinium Moiety as Potent Acetylcholinesterase Inhibitors: Design, Synthesis, Biological Evaluation and Docking Study
by: mehri abdollahi fard, et al.
Published: (2022-12-01)

Thiamine and Thiamine Pyrophosphate as Non-Competitive Inhibitors of Acetylcholinesterase—Experimental and Theoretical Investigations
by: Łukasz Szeleszczuk, et al.
Published: (2025-01-01)

Salacia fruticosa methanol extract pretreatment attenuates scopolamine-induced cognitive decline and Alzheimer's disease-related pathology in zebrafish
by: Praveen Kumar Pasala, et al.
Published: (2025-03-01)

Fluorometric and Colorimetric Biosensors for the Assay of Cholinesterase Inhibitors
by: Miroslav Pohanka
Published: (2025-04-01)

A Randomized Pilot Study of Four Dosing Schemes of Sublingual Methazolamide in Glaucoma Patients
by: Tan NE, et al.
Published: (2024-12-01)

Ketogenic Diet: Effects on Growth
by: J Gordon Millichap
Published: (2002-12-01)

Anticholinesterase activities from aqueous extract of different plant parts of Erica manipuliflora
by: Çiğdem Kuş, et al.
Published: (2017-12-01)

Exploring the binding potential of natural compounds to carbonic anhydrase of cyanobacteria through computer-based simulations
by: Archana Padhiary, et al.
Published: (2025-03-01)

An ureido-substituted benzenesulfonamide carbonic anhydrase inhibitor exerts a potent antitumor effect in vitro and in vivo
by: Giorgia Gazzaroli, et al.
Published: (2025-08-01)

Exploring novel of 1,2,4-triazolo[4,3-a]quinoxaline sulfonamide regioisomers as anti-diabetic and anti-Alzheimer agents with in-silico molecular docking simulation
by: Moustafa S. Abusaif, et al.
Published: (2025-06-01)

A novel thiazole-sulfonamide hybrid molecule as a promising dual tubulin/carbonic anhydrase IX inhibitor with anticancer activity
by: Hussam Elddin Nabeih Khasawneh, et al.
Published: (2025-06-01)

DFT-Based Elucidation and Evaluation of Selenium-Modified Tacrine Derivatives: Theoretical and Physicochemical Insights for Alzheimer’s Disease Therapy
by: Roberto Barbosa Morais, et al.
Published: (2025-06-01)

Novel coumarin chalcone derivatives: synthesis, docking, and antimicrobial evaluation
by: Sumita Kumari, et al.
Published: (2025-02-01)

Synthesis, antimicrobial evaluation, ADMET prediction, molecular docking and dynamics studies of pyridine and thiophene moiety-containing chalcones
by: Fahmida Akhter, et al.
Published: (2025-01-01)

Isolation of Pleurotus florida derived acetylcholinesterase inhibitor for the treatment of cognitive dysfunction in mice
by: Kudrat Randhawa, et al.
Published: (2021-07-01)

SMILES-based QSAR and molecular docking studies of chalcone analogues as potential anti-colon cancer
by: Abolfazl Askarzade, et al.
Published: (2025-02-01)

Use of connectivity index and simple topological parameters for estimating the inhibition potency of acetylcholinesterase
by: Ante Miličević, et al.
Published: (2022-04-01)