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 |
- 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
-
Inhibition of Ceramide Metabolism Key Enzymes and its Implication in Cell Physiology and Pathology
Current Enzyme Inhibition Genetic Features of MAPT, GRN, C9orf72 and CHCHD10 Gene Mutations in Chinese Patients with Frontotemporal Dementia
Current Alzheimer Research Targeting the BH3 Domain of Bcl-2 Family Proteins. A Brief History From Natural Products to Foldamers As Promising Cancer Therapeutic Avenues
Current Medicinal Chemistry Polyunsaturated Fatty Acids in Emerging Psychosis
Current Pharmaceutical Design Chemical Modification of Chitosan as a Gene Transporter
Current Organic Chemistry Attenuating Muscle Wasting: Cell and Gene Therapy Approaches
Current Genomics Nitric Oxide Homeostasis in Neurodegenerative Diseases
Current Alzheimer Research Implication of Oncogenic Signaling Pathways as a Treatment Strategy for Neurodegenerative Disorders – Contemporary Approaches
CNS & Neurological Disorders - Drug Targets MicroRNA: Novel Modulators of the Cholinergic Anti-Inflammatory Pathway
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry The Pivotal Role of Nitric Oxide: Effects on the Nervous and Immune Systems
Current Pharmaceutical Design RAGE, Diabetes, and the Nervous System
Current Molecular Medicine Changes in the Expression of the Alzheimers Disease-Associated Presenilin Gene in Drosophila Heart Leads to Cardiac Dysfunction
Current Alzheimer Research Computational Studies Applied to Linalool and Citronellal Derivatives Against Alzheimer's and Parkinson's Disorders: A Review with Experimental Approach
Current Neuropharmacology Design of New Drugs for the Treatment of Alzheimer’s Disease Based on Tacrine Structure
Current Drug Targets Disorder in Milk Proteins: α -Lactalbumin. Part A. Structural Properties and Conformational Behavior
Current Protein & Peptide Science The Developing Utility of Zebrafish Models for Cognitive Enhancers Research
Current Neuropharmacology The NOX1/4 Inhibitor GKT136901 as Selective and Direct Scavenger of Peroxynitrite
Current Medicinal Chemistry A Multicentre Italian Validation Study in Aging Adults with Down Syndrome and Other Forms of Intellectual Disabilities: Dementia Screening Questionnaire for Individuals with Intellectual Disabilities
Current Alzheimer Research AZT: An Old Drug with New Perspectives
Current Clinical Pharmacology Application of Contemporary Neuroproteomic Techniques in Unravelling Neurological Disorders
Current Protein & Peptide Science