Abstract
In the present paper, we describe the synthesis and biological evaluation for a series of novel 6,9-disubstituted 2-methyl-1,2,3,4,5,6-hexahydroazepino[4,3-b]indoles. These compounds represent unique bioisosteric analogues of Dimebon ™ with promising biological activity against a panel of various targets including some GPCR family members.
Keywords: Dimebon™, Inhibitor, 1,2,3,4,5,6-hexahydroazepino[4,3-b]indole, Alzheimer's disease, Parallel synthesis, GPCR, Analogues
Letters in Drug Design & Discovery
Title: Synthesis and Biological Evaluation of Novel Bioisosteric Analogues of Dimebon™
Volume: 7 Issue: 6
Author(s): Alexandre Vasilevich Ivachtchenko, Eugene Borisovich Frolov, Oleg Dmitrievich Mitkin, Sergey Evgenevich Tkachenko and Alexandre Khvat
Affiliation:
Keywords: Dimebon™, Inhibitor, 1,2,3,4,5,6-hexahydroazepino[4,3-b]indole, Alzheimer's disease, Parallel synthesis, GPCR, Analogues
Abstract: In the present paper, we describe the synthesis and biological evaluation for a series of novel 6,9-disubstituted 2-methyl-1,2,3,4,5,6-hexahydroazepino[4,3-b]indoles. These compounds represent unique bioisosteric analogues of Dimebon ™ with promising biological activity against a panel of various targets including some GPCR family members.
Export Options
About this article
Cite this article as:
Vasilevich Ivachtchenko Alexandre, Borisovich Frolov Eugene, Dmitrievich Mitkin Oleg, Evgenevich Tkachenko Sergey and Khvat Alexandre, Synthesis and Biological Evaluation of Novel Bioisosteric Analogues of Dimebon™, Letters in Drug Design & Discovery 2010; 7 (6) . https://dx.doi.org/10.2174/157018010791306579
DOI https://dx.doi.org/10.2174/157018010791306579 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
Related Journals
Related Books
- 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
-
Matrix Metalloproteinase-2 and Epidermal Growth Factor are Decreased in Platelets of Alzheimer Patients
Current Alzheimer Research Melatonin: Pharmacology, Functions and Therapeutic Benefits
Current Neuropharmacology Regulation of Ion Channels, Cellular Carriers and Na(+)/K(+)/ATPase by Janus Kinase 3
Current Medicinal Chemistry Protective Effects of Crocetin on Depression-like Behavior Induced by Immobilization in Rat
CNS & Neurological Disorders - Drug Targets Homology Modeling of Adenosine A2A Receptor and Molecular Docking for Exploration of Appropriate Potent Antagonists for Treatment of Parkinsons Disease
Current Aging Science Multi-Target Directed Compounds with Antioxidant and/or Anti- Inflammatory Properties as Potent Agents for Alzheimer’s Disease
Medicinal Chemistry Kinetic Study on the Effects of Extremely Low Frequency Electromagnetic Field on Catalase, Cytochrome P450 and Inducible Nitric Oxide Synthase in Human HaCaT and THP-1 Cell Lines
CNS & Neurological Disorders - Drug Targets Impact of Cytokines and Chemokines on Alzheimer’s Disease Neuropathological Hallmarks
Current Alzheimer Research Meet Our Editorial Board Member
CNS & Neurological Disorders - Drug Targets Amyloid β Accumulation Assessed with <sup>11</sup>C-Pittsburgh Compound B PET and Postmortem Neuropathology
Current Alzheimer Research Relevance of the Chronobiological and Non-chronobiological Actions of Melatonin for Enhancing Therapeutic Efficacy in Neurodegenerative Disorders
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery (Discontinued) Control and Role of Plateau Potential Properties in the Spinal Cord
Current Pharmaceutical Design Crosstalk between Gut Microbiota and Central Nervous System: A Focus on Alzheimer's Disease
Current Alzheimer Research Protein Glycation: An Old Villain is Shedding Secrets
Combinatorial Chemistry & High Throughput Screening Recent Patent Advances for Neurodegenerative Disorders and its Treatment
Recent Patents on Drug Delivery & Formulation Aging Affects Nicotinic Acetylcholine Receptors in Brain
Central Nervous System Agents in Medicinal Chemistry Diversity and Variability of the Effects of Nicotine on Different Cortical Regions of the Brain. Therapeutic and Toxicological Implications
Central Nervous System Agents in Medicinal Chemistry Mood, Memory and Movement: An Age-Related Neurodegenerative Complex?
Current Aging Science The Bax Inhibitor-1 (BI-1) Family in Apoptosis and Tumorigenesis
Current Molecular Medicine New Prospectives in the Delivery of Galantamine for Elderly Patients Using the IntelliDrug Intraoral Device: In Vivo Animal Studies
Current Pharmaceutical Design