Abstract
Pd/C-Cu mediated alternative and one-pot method has been developed for the synthesis of (Z)-3- methyleneisoindolin-1-ones as potential inhibitors of PDE4. The methodology involved coupling-cyclization of obromobenzamides with a range of terminal alkynes in a single pot to afford the target compounds in acceptable yields. Some of these compounds showed encouraging inhibition of PDE4 when tested in vitro that was supported by in silico docking studies.
Keywords: Alkynes, Pd/C, coupling, 3-methyleneisoindolin-1-ones.
Letters in Drug Design & Discovery
Title:Pd/C-mediated Synthesis of 3-methyleneisoindolin-1-ones: Biological and Theoretical Study of their PDE4 Inhibition
Volume: 11 Issue: 10
Author(s): Suryadevara Vijayavardhini, Dandela Rambabu, Vegendla Anuradha, Ravikumar Kapavarapu, Mandava Venkata Basaveswara Rao and Manojit Pal
Affiliation:
Keywords: Alkynes, Pd/C, coupling, 3-methyleneisoindolin-1-ones.
Abstract: Pd/C-Cu mediated alternative and one-pot method has been developed for the synthesis of (Z)-3- methyleneisoindolin-1-ones as potential inhibitors of PDE4. The methodology involved coupling-cyclization of obromobenzamides with a range of terminal alkynes in a single pot to afford the target compounds in acceptable yields. Some of these compounds showed encouraging inhibition of PDE4 when tested in vitro that was supported by in silico docking studies.
Export Options
About this article
Cite this article as:
Vijayavardhini Suryadevara, Rambabu Dandela, Anuradha Vegendla, Kapavarapu Ravikumar, Basaveswara Rao Venkata Mandava and Pal Manojit, Pd/C-mediated Synthesis of 3-methyleneisoindolin-1-ones: Biological and Theoretical Study of their PDE4 Inhibition, Letters in Drug Design & Discovery 2014; 11 (10) . https://dx.doi.org/10.2174/1570180811666140717190618
DOI https://dx.doi.org/10.2174/1570180811666140717190618 |
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
-
Identification of Functional Peptides from Natural and Synthetic Products on Their Anticancer Activities by Tumor Targeting
Current Medicinal Chemistry Development of Anti-HIV Agents Targeting Dynamic Supramolecular Mechanism: Entry and Fusion Inhibitors Based on CXCR4/CCR5 Antagonists and gp41-C34-Remodeling Peptides
Current HIV Research Expression and Function of Angiomodulating Cytokines in Rheumatoid Arthritis and Experimental Arthritis: Important Therapeutic Targets
Current Immunology Reviews (Discontinued) Low Lymphocyte Count and Cardiovascular Diseases
Current Medicinal Chemistry Dendritic Cells for Active Anti-Cancer Immunotherapy: Targeting Activation Pathways Through Genetic Modification
Endocrine, Metabolic & Immune Disorders - Drug Targets Bioinformatic Screening of Autoimmune Disease Genes and Protein Structure Prediction with FAMS for Drug Discovery
Protein & Peptide Letters Ligand Based-Pharmacophore Modeling and Extended Bi oactivity Prediction for Salinosporamide A, B and C from Marine Actino mycetes Salinispora tropica
Combinatorial Chemistry & High Throughput Screening Anti-Interleukin-6 Therapy for Crohns Disease
Current Pharmaceutical Design The Capability to Forecast Response to Therapy with Regard to The Time and Intensity of The Inflammatory Process in vitro in Dermal Fibroblasts Induced by IL-12
Current Pharmaceutical Biotechnology DNA Methylation in Osteoarthritis
Current Genomics MIF and the Genetic Basis of Macrophage Responsiveness
Current Immunology Reviews (Discontinued) Role of NADPH Oxidase in Hypertension and Diabetic Nephropathy
Current Hypertension Reviews Local Treatment for Lymphoid Malignancies of the Eye
Anti-Cancer Agents in Medicinal Chemistry Targeting the Phosphatidylinositol 3-Kinase/AKT Pathway for the Treatment of Multiple Myeloma
Current Medicinal Chemistry Is Atorvastatin Superior to Other Statins? Analysis of the Clinical Trials with Atorvastatin Having Cardiovascular Endpoints
Reviews on Recent Clinical Trials Therapeutic Implications of Superoxide Dismutase And Its Importance in Kinase Drug Discovery
Current Topics in Medicinal Chemistry Biologics in Inflammatory and Immunomediated Arthritis
Current Pharmaceutical Biotechnology Pembrolizumab-Induced Seronegative Arthritis and Fasciitis in a Patient with Lung Adenocarcinoma
Current Drug Safety Drug Discovery and Design for Complex Diseases through QSAR Computational Methods
Current Pharmaceutical Design Quantitative Structure-Activity Relationship Studies on Some Novel Anti- HIV Thiourea Derivatives with Cytotoxicity Data (CC50) in MT-4 Cells
Letters in Drug Design & Discovery