Abstract
A series of novel fluorinated heterocyclic hybrid molecules based on triazole & quinoxaline scaffold were designed, synthesized and evaluated for inhibition of Plasmodium falciparum, a virulent human malaria parasite. Mono and bis triazole tagged quinoxaline analogs were synthesized by propargylation of 6-amino quinoxaline followed by click reaction with various substituted aromatic azides under uncertain reaction conditions. The newly synthesized molecules were assessed for antimalarial activity and three of the analogs were identified as promising leads which killed parasites with IC50 values <10 μM and showed 27-70 selective indices.
Keywords: Antimalarials, click reaction, hybrid molecules, plasmodium, quinoxalines, triazoles.
Letters in Drug Design & Discovery
Title:Design, Synthesis and Biological Evaluation of Novel Fluorinated Heterocyclic Hybrid Molecules Based on Triazole & Quinoxaline Scaffolds Lead to Highly Potent Antimalarials and Antibacterials
Volume: 12 Issue: 5
Author(s): Adimulam Chandra Shekhar, Boddupally Pedda Venkat Lingaiah, Pamulaparthy Shanthan Rao, Banda Narsaiah, Aparna Devi Allanki and Puran Singh Sijwali
Affiliation:
Keywords: Antimalarials, click reaction, hybrid molecules, plasmodium, quinoxalines, triazoles.
Abstract: A series of novel fluorinated heterocyclic hybrid molecules based on triazole & quinoxaline scaffold were designed, synthesized and evaluated for inhibition of Plasmodium falciparum, a virulent human malaria parasite. Mono and bis triazole tagged quinoxaline analogs were synthesized by propargylation of 6-amino quinoxaline followed by click reaction with various substituted aromatic azides under uncertain reaction conditions. The newly synthesized molecules were assessed for antimalarial activity and three of the analogs were identified as promising leads which killed parasites with IC50 values <10 μM and showed 27-70 selective indices.
Export Options
About this article
Cite this article as:
Chandra Shekhar Adimulam, Pedda Venkat Lingaiah Boddupally, Shanthan Rao Pamulaparthy, Narsaiah Banda, Devi Allanki Aparna and Sijwali Puran Singh, Design, Synthesis and Biological Evaluation of Novel Fluorinated Heterocyclic Hybrid Molecules Based on Triazole & Quinoxaline Scaffolds Lead to Highly Potent Antimalarials and Antibacterials, Letters in Drug Design & Discovery 2015; 12 (5) . https://dx.doi.org/10.2174/1570180812666141111235301
DOI https://dx.doi.org/10.2174/1570180812666141111235301 |
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
-
Genomic Expression in the Epileptogenic Hippocampus and Psychiatric Co-Morbidities
Current Psychiatry Reviews Inhalation Gases or Gaseous Mediators As Neuroprotectants for Cerebral Ischaemia
Current Drug Targets Immune Aging and Autoimmune Diseases in Children
Current Immunology Reviews (Discontinued) CD20-based Immunotherapy of B-cell Derived Hematologic Malignancies
Current Cancer Drug Targets A Review of Preclinical Research Demonstrating that Drug and Non-Drug ReinforcersDifferentially Affect Behavior
Current Drug Abuse Reviews Small Molecules for the Activation of Human γ δ T Cell Responses Against Infection
Recent Patents on Anti-Infective Drug Discovery Fanconi Anemia Proteins, DNA Interstrand Crosslink Repair Pathways, and Cancer Therapy
Current Cancer Drug Targets Blood Biomarkers for the Differentiation of Cardiac Ischemic Stroke Subtypes: A Systematic Review
Cardiovascular & Hematological Disorders-Drug Targets A Knock-Down Cell-Based Study for the Functional Analysis of Chloride Intracellular Channel 1 (CLIC1): Integrated Proteomics and Microarray Study
Protein & Peptide Letters Selectins as Targets in Inflammatory Diseases
Current Medicinal Chemistry - Anti-Inflammatory & Anti-Allergy Agents Natural DNA Intercalators as Promising Therapeutics for Cancer and Infectious Diseases
Current Cancer Drug Targets Strategies to Improve the Killing of Tumors Using Temozolomide: Targeting the DNA Repair Protein MGMT
Current Medicinal Chemistry Molecule of the Month
Current Topics in Medicinal Chemistry Foreword
Recent Patents on CNS Drug Discovery (Discontinued) Cosignaling Molecules Around LIGHT-HVEM-BTLA: From Immune Activation to Therapeutic Targeting
Current Molecular Medicine Update on Targets of Biologic Therapies for Rheumatoid Arthritis
Current Rheumatology Reviews Meet Our Editorial Board Member:
Current Drug Metabolism Therapeutic Manipulation of the Immune System: Enhancement of Innate and Adaptive Mucosal Immunity
Current Pharmaceutical Design Endothelial Dysfunction in Renal Failure: Current Update
Current Medicinal Chemistry Reacting to Stress: Radical Cellular Pathways for Novel Drug Development
Current Neurovascular Research