Abstract
Background: Dihydropyrimidinone is considered as a pharmacophoric skeleton in many drug discovery programmes. To explore the activity of dihydropyrimidines, we regioselectively synthesized some of the substituted mannich bases of dihydropyrimidinone (DHPM) analogues regioselectively with fluoroquinolones (Ciprofloxacin). Methods: Regioselectivity in these structures is achieved by the influence of weak base like potassium carbonate and synthesized some novel dihydropyrimidine N- and O-Mannich bases of ciprofloxacin (3a-j, 4a-g) using microwave technology. All the synthesized molecules have been evaluated for their antiviral activity against hepatitis C, hepatitis B, vaccinia, cowpox, severe acute respiratory syndrome, West Nile, dengue, Venezuelan equine encephalitis viruses, Flu A (H1N1, H3N2 and H5N1) and Flu B viral strains as well as for their cytotoxicity using standard protocols. Results: An attempt was made to interpret the structure activity relation of compounds with their antiviral activity data. Compounds 3a, 3e, 3f, 4e, 4g were found to be active against Flu A (H1N1), TCRV, hepatitis B, yellow fever, vaccinia virus respectively. Conclusion: Some of the synthesized compounds exhibited potent activity against some viral strains. Out of O- and N-mannich bases, O-mannich bases were found to be more potent with high selectivity index.
Keywords: Antiviral activity, dihydropyrimidinones, hepatitis B, influenza virus A (H1N1), microwave technology, regioselectivity, TCRV, vaccinia virus, yellow fever.
Anti-Infective Agents
Title:Synthesis and Antiviral Activity of Dihydropyrimidines - Ciprofloxacin Mannich bases Against Various Viral Strains
Volume: 13 Issue: 2
Author(s): Rajasekhar R. Alavala, Umasankar Kulandaivelu, Pochaiah Bonagiri, Shireesha Boyapati, Venkatesan Jayaprakash and Ananda T. Subramaniam
Affiliation:
Keywords: Antiviral activity, dihydropyrimidinones, hepatitis B, influenza virus A (H1N1), microwave technology, regioselectivity, TCRV, vaccinia virus, yellow fever.
Abstract: Background: Dihydropyrimidinone is considered as a pharmacophoric skeleton in many drug discovery programmes. To explore the activity of dihydropyrimidines, we regioselectively synthesized some of the substituted mannich bases of dihydropyrimidinone (DHPM) analogues regioselectively with fluoroquinolones (Ciprofloxacin). Methods: Regioselectivity in these structures is achieved by the influence of weak base like potassium carbonate and synthesized some novel dihydropyrimidine N- and O-Mannich bases of ciprofloxacin (3a-j, 4a-g) using microwave technology. All the synthesized molecules have been evaluated for their antiviral activity against hepatitis C, hepatitis B, vaccinia, cowpox, severe acute respiratory syndrome, West Nile, dengue, Venezuelan equine encephalitis viruses, Flu A (H1N1, H3N2 and H5N1) and Flu B viral strains as well as for their cytotoxicity using standard protocols. Results: An attempt was made to interpret the structure activity relation of compounds with their antiviral activity data. Compounds 3a, 3e, 3f, 4e, 4g were found to be active against Flu A (H1N1), TCRV, hepatitis B, yellow fever, vaccinia virus respectively. Conclusion: Some of the synthesized compounds exhibited potent activity against some viral strains. Out of O- and N-mannich bases, O-mannich bases were found to be more potent with high selectivity index.
Export Options
About this article
Cite this article as:
R. Alavala Rajasekhar, Kulandaivelu Umasankar, Bonagiri Pochaiah, Boyapati Shireesha, Jayaprakash Venkatesan and T. Subramaniam Ananda, Synthesis and Antiviral Activity of Dihydropyrimidines - Ciprofloxacin Mannich bases Against Various Viral Strains, Anti-Infective Agents 2015; 13 (2) . https://dx.doi.org/10.2174/221135251302151029111113
DOI https://dx.doi.org/10.2174/221135251302151029111113 |
Print ISSN 2211-3525 |
Publisher Name Bentham Science Publisher |
Online ISSN 2211-3533 |
- 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
- Announcements
Related Articles
-
Anti-Viral
Current Bioactive Compounds Antimicrobial Effect of Garlic (Allium sativum)
Recent Patents on Anti-Infective Drug Discovery Immune Senescence and Vaccination in the Elderly
Current Topics in Medicinal Chemistry Synthesis and Biological Evaluation of a Series of 4-(arylamido/imidoalkyl)- 5-(arylideno- 4-oxo-2-thio-imidazolidinyl)-N-(methyl-phenyl-imino) Acridinium Iodides as Potential Antiviral Agents
Letters in Drug Design & Discovery Endotoxin, TLR4 Signaling and Vascular Inflammation: Potential Therapeutic Targets in Cardiovascular Disease
Current Pharmaceutical Design Altering the Tropism of Lentiviral Vectors through Pseudotyping
Current Gene Therapy Progressive Supranuclear Palsy: What Do We Know About it?
Current Medicinal Chemistry Improving Cognitive Outcome in Cerebral Malaria: Insights from Clinical and Experimental Research
Central Nervous System Agents in Medicinal Chemistry Enhancing the Delivery of Anti Retroviral Drug “Saquinavir” Across the Blood Brain Barrier Using Nanoparticles
Current HIV Research The Therapeutic Potential of Melatonin in Neurological Disorders
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery (Discontinued) The Urokinase Receptor in the Central Nervous System
CNS & Neurological Disorders - Drug Targets Gene Therapy to Improve Pancreatic Islet Transplantation for Type 1 Diabetes Mellitus
Current Diabetes Reviews Mutations of mtDNA in some Vascular and Metabolic Diseases
Current Pharmaceutical Design Sodium Lauryl Sulfate, a Microbicide Effective Against Enveloped and Nonenveloped Viruses
Current Drug Targets T2/FLAIR Hyperintensity in Mesial Temporal Lobe: Challenging Differential Diagnosis
Current Medical Imaging What Animal Models are Best to Test Novel Rheumatoid Arthritis Therapies?
Current Rheumatology Reviews Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications
Current Neuropharmacology Impact of Latent Viral Infections in Mechanically Ventilated Patients
Current Respiratory Medicine Reviews Computational Approaches for the Design of Mosquito Repellent Chemicals
Current Medicinal Chemistry Potential Use of Nanomedicine for Drug Delivery Across the Blood-Brain Barrier in Healthy and Diseased Brain
CNS & Neurological Disorders - Drug Targets