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
-
Recent Patents in Bone Graft Substitute for Bone, Tendon, and Ligament Reconstruction
Recent Patents on Biomedical Engineering (Discontinued) Natural Products Based Anticancer Agents
Mini-Reviews in Organic Chemistry On the Structural Basis of the Hypertensive Properties of Angiotensin II: A Solved Mystery or a Controversial Issue?
Current Topics in Medicinal Chemistry Ligand-Based Peptide Design and Combinatorial Peptide Libraries to Target G Protein-Coupled Receptors
Current Pharmaceutical Design Peptide-Containing Block Copolymers: Synthesis and Potential Applications of Bio-Mimetic Materials
Current Organic Chemistry Medical Management of the Diabetic Patient with Coronary Artery Disease
Current Pharmaceutical Design Transcatheter Aortic Valve Technology: Current State
Recent Patents on Biomedical Engineering (Discontinued) Polyphenols and Cardiovascular Disease: A Critical Summary of the Evidence
Mini-Reviews in Medicinal Chemistry Subject Index To Volume 7
Current Pharmaceutical Design Model Systems for Pulmonary Infectious Diseases: Paradigms of Anthrax and Tuberculosis
Current Topics in Medicinal Chemistry Recent Advances in the Discovery of HIF-1α-p300/CBP Inhibitors as Anti-Cancer Agents
Mini-Reviews in Medicinal Chemistry The Pleiotropic Effects of PPARs on Vascular Cells and Angiogenesis: Implications for Tissue Engineering
Current Stem Cell Research & Therapy Diabetes Mellitus as a Risk Factor for Cancer: Stress or Viral Etiology?
Infectious Disorders - Drug Targets Screening of Antihypertensive Drugs for Osteoclastic Acid Secretion and Bone Resorption by Acridine Orange
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Flavonoids as Anticancer Agents: Recent Progress and State of the Art?
Current Organic Chemistry ATP-Sensitive Potassium Channels
Current Pharmaceutical Design Structure-Based Virtual Ligand Screening: Recent Success Stories
Combinatorial Chemistry & High Throughput Screening Antineoplastic Activities, Apoptotic Mechanism of Action and Structural Properties of a Novel Silver(I) Chelate
Current Medicinal Chemistry Type A and B Monoamine Oxidase in Age-Related Neurodegenerative Disorders: Their Distinct Roles in Neuronal Death and Survival
Current Topics in Medicinal Chemistry The Etiology of Hypertension in the Metabolic Syndrome Part Four: The Systemic Perspective – The Role of the Neuroendocrine and Immune Systems,and the Challenge of Integration
Current Vascular Pharmacology