Abstract
A new series of phenyl- and heteryl acetamidines were synthesized and evaluated as inhibitors of nitric oxide synthases (NOS). While the N-substitution of the acetamidine moiety with different heterocycles appears to completely destroy the activity, linking the phenyl core preserves it. Moreover, it was observed a strong dependence of the phenylacetamidines potency of action from the length of the alkyl chain that connects the aromatic ring to the acetamidine moiety.
Keywords: Nitric oxide, Nitric oxide synthase, Selective inducible NOS inhibitors, Acetamidines, heterocycles, inorganic, neurodegenerative diseases, cytokines, polysaccharides, amino acid
Medicinal Chemistry
Title:Selective Inhibition of Inducible Nitric Oxide Synthase by Derivatives of Acetamidine
Volume: 8 Issue: 6
Author(s): Cristina Maccallini, Antonia Patruno, Alessandra Ammazzalorso, Barbara De Filippis, Marialuigia Fantacuzzi, Sara Franceschelli, Letizia Giampietro, Simona Masella, Maria Luisa Tricca and Rosa Amoroso
Affiliation:
Keywords: Nitric oxide, Nitric oxide synthase, Selective inducible NOS inhibitors, Acetamidines, heterocycles, inorganic, neurodegenerative diseases, cytokines, polysaccharides, amino acid
Abstract: A new series of phenyl- and heteryl acetamidines were synthesized and evaluated as inhibitors of nitric oxide synthases (NOS). While the N-substitution of the acetamidine moiety with different heterocycles appears to completely destroy the activity, linking the phenyl core preserves it. Moreover, it was observed a strong dependence of the phenylacetamidines potency of action from the length of the alkyl chain that connects the aromatic ring to the acetamidine moiety.
Export Options
About this article
Cite this article as:
Maccallini Cristina, Patruno Antonia, Ammazzalorso Alessandra, De Filippis Barbara, Fantacuzzi Marialuigia, Franceschelli Sara, Giampietro Letizia, Masella Simona, Luisa Tricca Maria and Amoroso Rosa, Selective Inhibition of Inducible Nitric Oxide Synthase by Derivatives of Acetamidine, Medicinal Chemistry 2012; 8 (6) . https://dx.doi.org/10.2174/1573406411208060991
DOI https://dx.doi.org/10.2174/1573406411208060991 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
- 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
-
Regulators of G Protein Signaling: Potential Drug Targets for Controlling Cardiovascular and Immune Function
Current Drug Targets - Immune, Endocrine & Metabolic Disorders Combretastatin A-4 Analogs as Anticancer Agents
Mini-Reviews in Medicinal Chemistry Recent Advances of Small Molecule Focal Adhesion Kinase (FAK) Inhibitors as Promising Anticancer Therapeutics
Current Medicinal Chemistry The Drug Targeting and Delivery Approach Applied to Pt-Antitumour Complexes. A Coordination Point of View
Current Medicinal Chemistry TGF Beta Inhibition for Cancer Therapy
Current Cancer Drug Targets Should we Target Allergen Protease Activity to Decrease the Burden of Allergic Airway Inflammation?
Inflammation & Allergy - Drug Targets (Discontinued) New Molecular Avenues in Parkinson ’ s Disease Therapy
Current Topics in Medicinal Chemistry Vascular Effects of Ambient Pollutant Particles and Metals
Current Vascular Pharmacology Small Molecule Inhibitors of PKCθ as Potential Antiinflammatory Therapeutics
Current Topics in Medicinal Chemistry p53: A Guide to Apoptosis
Current Cancer Drug Targets The Effects of Newer Beta-Adrenoceptor Antagonists on Vascular Function in Cardiovascular Disease
Current Vascular Pharmacology Dual Acting Antihistaminergic Agents
Mini-Reviews in Medicinal Chemistry Oligodendrocyte Development and Myelination in Neurodevelopment: Molecular Mechanisms in Health and Disease
Current Pharmaceutical Design Energy Balance and Carcinogenesis: Underlying Pathways and Targets for Intervention
Current Cancer Drug Targets Naturally Occurring NF-κB Inhibitors
Mini-Reviews in Medicinal Chemistry An Overview of the Current and Novel Drugs for Alzheimers Disease with Particular Reference to Anti-Cholinesterase Compounds
Current Pharmaceutical Design The Prevention of Preterm Labour - Corticotropin Releasing Hormone Type 1 Receptors as a Target for Drug Design and Development
Mini-Reviews in Medicinal Chemistry Ecto-Nucleotidase Inhibitors: Recent Developments in Drug Discovery
Mini-Reviews in Medicinal Chemistry Tyrosine Kinase Inhibitor as a new Therapy for Ischemic Stroke and other Neurologic Diseases: is there any Hope for a Better Outcome?
Current Neuropharmacology Identification of Novel 5,6-Dimethoxyindan-1-one Derivatives as Antiviral Agents
Medicinal Chemistry