Abstract
N'-Benzylidene-2-[[5-(phenylamino)-1,3,4-thiadiazol-2-yl]thio]acetohydrazide derivatives (5a-p) were synthesized to screen for their AChE, BuChE and LOX inhibitory activity. The CCK-8 assay was also carried out to determine their cytotoxicity against NIH/3T3 cells. The most potent AChE inhibitors were found as compounds 5m (49.79% ± 3.08) and 5p (42.39% ± 3.19), whereas the most potent BuChE inhibitor was found as compound 5d (35.15% ± 2.21). Among these derivatives, N'-(3-methoxybenzylidene)-2-[[5-(phenylamino)-1,3,4-thiadiazol-2-yl]thio]acetohydrazide (5p) can be considered as the most promising AChE inhibitor due to its low cytotoxicity to NIH/3T3 cells (IC50 > 500 µg/mL). N'-(4- Methoxybenzylidene)-2-[[5-(phenylamino)-1,3,4-thiadiazol-2-yl]thio]a-cetohydrazide (5n) exhibited weak inhibition on LOX (%20.65 ± 0.08), whilst the other compounds were not active.
Keywords: Acetylcholinesterase, butyrylcholinesterase, lipoxygenase, thiadiazole.
Letters in Drug Design & Discovery
Title:Synthesis and In vitro Evaluation of Thiadiazole Derivatives as AChE, Bu- ChE and LOX Inhibitors
Volume: 11 Issue: 9
Author(s): Mehlika Dilek Altintop, Ahmet Ozdemir, Usama Abu Mohsen, Halide Edip Temel, Gulsen Akal n Ciftci and Zafer Asim Kaplancikli
Affiliation:
Keywords: Acetylcholinesterase, butyrylcholinesterase, lipoxygenase, thiadiazole.
Abstract: N'-Benzylidene-2-[[5-(phenylamino)-1,3,4-thiadiazol-2-yl]thio]acetohydrazide derivatives (5a-p) were synthesized to screen for their AChE, BuChE and LOX inhibitory activity. The CCK-8 assay was also carried out to determine their cytotoxicity against NIH/3T3 cells. The most potent AChE inhibitors were found as compounds 5m (49.79% ± 3.08) and 5p (42.39% ± 3.19), whereas the most potent BuChE inhibitor was found as compound 5d (35.15% ± 2.21). Among these derivatives, N'-(3-methoxybenzylidene)-2-[[5-(phenylamino)-1,3,4-thiadiazol-2-yl]thio]acetohydrazide (5p) can be considered as the most promising AChE inhibitor due to its low cytotoxicity to NIH/3T3 cells (IC50 > 500 µg/mL). N'-(4- Methoxybenzylidene)-2-[[5-(phenylamino)-1,3,4-thiadiazol-2-yl]thio]a-cetohydrazide (5n) exhibited weak inhibition on LOX (%20.65 ± 0.08), whilst the other compounds were not active.
Export Options
About this article
Cite this article as:
Altintop Dilek Mehlika, Ozdemir Ahmet, Mohsen Abu Usama, Temel Edip Halide, Ciftci Akal n Gulsen and Kaplancikli Asim Zafer, Synthesis and In vitro Evaluation of Thiadiazole Derivatives as AChE, Bu- ChE and LOX Inhibitors, Letters in Drug Design & Discovery 2014; 11 (9) . https://dx.doi.org/10.2174/1570180811666140529004517
DOI https://dx.doi.org/10.2174/1570180811666140529004517 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Oxidant/Antioxidant Imbalance and the Risk of Alzheimer's Disease
Current Alzheimer Research Blue-Enriched Lighting for Older People Living in Care Homes: Effect on Activity, Actigraphic Sleep, Mood and Alertness
Current Alzheimer Research The Intranasal Administration of 1-Methyl-4-Phenyl-1,2,3,6-Tetrahydropyridine (MPTP): A New Rodent Model to Test Palliative and Neuroprotective Agents for Parkinsons disease
Current Pharmaceutical Design Recent Patents on Polymeric Scaffolds for Tissue Engineering
Recent Patents on Biomedical Engineering (Discontinued) The Effects of Antihypertensive Therapy on Haemostatic Parameters
Current Pharmaceutical Design Secondary Hypertension: The Ways of Management
Current Vascular Pharmacology Is Human Immunodeficiency Virus-Mediated Dementia an Autophagic Defect that Leads to Neurodegeneration?
CNS & Neurological Disorders - Drug Targets Retrospective Results on the Treatment of Chronic Hepatitis C with Different Interferon Regimes in a General Hospital
Current Drug Therapy ABC Subfamily D Proteins and Very Long Chain Fatty Acid Metabolism as Novel Targets in Adrenoleukodystrophy
Current Drug Targets Conference Report: 10th Clinical Trials on Alzheimer's Disease (CTAD), Boston MA, USA, November 1-4, 2017
CNS & Neurological Disorders - Drug Targets Proteases Essential for Human Influenza Virus Entry into Cells and Their Inhibitors as Potential Therapeutic Agents
Current Pharmaceutical Design Alzheimers Disease-Associated Neurotoxic Mechanisms and Neuroprotective Strategies
Current Drug Targets - CNS & Neurological Disorders Metabolic Syndrome and Non-Cardiac Vascular Diseases: An Update from Human Studies
Current Pharmaceutical Design The Effect of TNFα-Inhibitors on Cardiovascular Events in Patients with Rheumatoid Arthritis: An Updated Systematic Review of the Literature
Current Rheumatology Reviews Treatment of Cognitive Impairment in Schizophrenia: Potential Value of Phosphodiesterase Inhibitors in Prefrontal Dysfunction
Current Pharmaceutical Design Effects of Snake Venom Polypeptides on Central Nervous System
Central Nervous System Agents in Medicinal Chemistry Fyn Kinase in Brain Diseases and Cancer: The Search for Inhibitors
Current Medicinal Chemistry Editorial [Hot topic: Polyunsaturated Fatty Acids and Human Health: A Critical Appraisal of the Evidence (Executive Editor: Antonio Cherubini)]
Current Pharmaceutical Design Subject Index to Volume 1
Current Alzheimer Research Induction of Molecular Chaperones as a Therapeutic Strategy for the Polyglutamine Diseases
Current Pharmaceutical Biotechnology