Abstract
Cholinesterase plays a vital role in the decline of cholinergic transmission and thus can contribute to the development of Alzheimer’s disease (AD). Thus, compounds that can inhibit acetylcholinesterase (AChe) and butyrylcholinesterase (BuChe) are the potential drugs for the treatment of AD. A series of novel pyrrolopyrimidine derivatives was synthesized and evaluated for their inhibitory activity against cholinesterase by Ellman method. Among the ten newly synthesized compounds, 4-(4-((4-(difluoromethoxy)phenyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)benzoate was the most potent molecule identified with the IC50 values of 18 µM and 17 µM on AChe and BuChe respectively.
Keywords: Acetylcholinesterase, alzheimer’s disease, butyrylcholinesterase, cholinergic transmission, inhibition, pyrrolopyrimidine.
Letters in Drug Design & Discovery
Title:Synthesis and Cholinesterase Inhibition Activity of New Pyrrolopyrimidine Derivatives
Volume: 11 Issue: 10
Author(s): Rangaswamy Roopashree, Toreshettahally Ramesh Swaroop, Swamy Jagadish, Chakrabhavi Dhananjaya Mohan and Kanchugarakoppal Subbegowda Rangappa
Affiliation:
Keywords: Acetylcholinesterase, alzheimer’s disease, butyrylcholinesterase, cholinergic transmission, inhibition, pyrrolopyrimidine.
Abstract: Cholinesterase plays a vital role in the decline of cholinergic transmission and thus can contribute to the development of Alzheimer’s disease (AD). Thus, compounds that can inhibit acetylcholinesterase (AChe) and butyrylcholinesterase (BuChe) are the potential drugs for the treatment of AD. A series of novel pyrrolopyrimidine derivatives was synthesized and evaluated for their inhibitory activity against cholinesterase by Ellman method. Among the ten newly synthesized compounds, 4-(4-((4-(difluoromethoxy)phenyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)benzoate was the most potent molecule identified with the IC50 values of 18 µM and 17 µM on AChe and BuChe respectively.
Export Options
About this article
Cite this article as:
Roopashree Rangaswamy, Ramesh Swaroop Toreshettahally, Jagadish Swamy, Dhananjaya Mohan Chakrabhavi and Subbegowda Rangappa Kanchugarakoppal, Synthesis and Cholinesterase Inhibition Activity of New Pyrrolopyrimidine Derivatives, Letters in Drug Design & Discovery 2014; 11 (10) . https://dx.doi.org/10.2174/1570180811666140704171902
DOI https://dx.doi.org/10.2174/1570180811666140704171902 |
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
-
Relationship Between Cigarette Smoking and Other Coronary Risk Factors in Atherosclerosis: Risk of Cardiovascular Disease and Preventive Measures
Current Pharmaceutical Design Classic β-Amyloid Deposits Cluster Around Large Diameter Blood Vessels Rather than Capillaries in Sporadic Alzheimers Disease
Current Neurovascular Research Anti-Chlamydophila pneumoniae Antibodies as Associated Factor for Carotid Atherosclerosis in Patients with AIDS
Current HIV Research The Serum Protein and Lipid Oxidation Marker Levels in Alzheimers Disease and Effects of Cholinesterase Inhibitors and Antipsychotic Drugs Therapy
Current Alzheimer Research Nitric Oxide in Asthma Therapy
Current Pharmaceutical Design Stroke in Women - Oral Contraception, Pregnancy, and Hormone Replacement Therapy
Current Vascular Pharmacology Platelets and Platelet Interaction with Progenitor Cells in Vascular Homeostasis and Inflammation
Current Vascular Pharmacology Expression and Function of Anti-Inflammatory Interleukins: The Other Side of the Vascular Response to Injury
Current Vascular Pharmacology Impact of the Emulsification-Diffusion Method on the Development of Pharmaceutical Nanoparticles
Recent Patents on Drug Delivery & Formulation Prognostic Parameters for Symptomatic Intracranial Hemorrhage after Intravenous Thrombolysis in Acute Ischemic Stroke in an Asian Population
Current Neurovascular Research Bleomycin and its Role in Inducing Apoptosis and Senescence in Lung Cells - Modulating Effects of Caveolin-1
Current Cancer Drug Targets Current Status of Hormone Replacement Therapy in Post Menopausal Women
Current Drug Therapy Bruton Kinase Inhibitors in Chronic Lymphocytic Leukemia
Anti-Cancer Agents in Medicinal Chemistry Homocysteine and Heart Failure: An Overview
Recent Patents on Cardiovascular Drug Discovery Withdrawal Notice: Atrial Fibrillation and Hypertension: “Quo Vadis”
Current Hypertension Reviews Nutraceuticals for Metabolic Syndrome Management: From Laboratory to Benchside
Current Vascular Pharmacology Is the Hepatic Factor a miRNA that Maintains the Integrity of Pulmonary Microvasculature by Inhibiting the Vascular Endothelial Growth Factor?
Current Cardiology Reviews Relationship between Augmentation Index and Wall Thickening Fraction during Hypotension in an Animal Model of Myocardial Ischemia-Reperfusion and Heart Failure
Current Hypertension Reviews <i>Ajuga</i> L.: A Systematic Review on Chemical Composition, Phytopharmacological and Biological Potential
Current Bioactive Compounds Editorial (Thematic Issue: Current Research, Knowledge and Controversies on High Density Lipoprotein)
Current Medicinal Chemistry