Abstract
Ten 1-benzenesulfonyl-1,2,3,4-tetrahydroquinoline (BSTHQ) were synthesized and characterized and their antiprotozoal activities were investigated. This small library was designed by combining two chemical moieties that are known to be biologically active by itself. The BS group seems to be favorable for the antiparasitic activity, since the derivatives presented lower IC50 value than the precursor heterocycle. Most compounds were moderately active against T cruzi, but 3 showed a promising IC50 value (9.76μM) with low cytotoxicity (L6). Also, 3, 6 and 9 showed interesting activity and reasonable selectivity against P. falciparum. These derivatives are considered as lead scaffolds and merit further exploration through structure optimization.
Keywords: Antiparasitic, Benzenesulfonyl, Tetrahydroquinolines, Stereoelectronic Properties
Letters in Drug Design & Discovery
Title: Design, Synthesis and 3-D Characterization of 1-Benzenesulfonyl-1,2,3,4- Tetrahydroquinolines as Lead Scaffold for Antiparasitic Drug
Volume: 7 Issue: 6
Author(s): R.J. Pagliero, A.B. Pierini, R. Brun and M.R. Mazzieri
Affiliation:
Keywords: Antiparasitic, Benzenesulfonyl, Tetrahydroquinolines, Stereoelectronic Properties
Abstract: Ten 1-benzenesulfonyl-1,2,3,4-tetrahydroquinoline (BSTHQ) were synthesized and characterized and their antiprotozoal activities were investigated. This small library was designed by combining two chemical moieties that are known to be biologically active by itself. The BS group seems to be favorable for the antiparasitic activity, since the derivatives presented lower IC50 value than the precursor heterocycle. Most compounds were moderately active against T cruzi, but 3 showed a promising IC50 value (9.76μM) with low cytotoxicity (L6). Also, 3, 6 and 9 showed interesting activity and reasonable selectivity against P. falciparum. These derivatives are considered as lead scaffolds and merit further exploration through structure optimization.
Export Options
About this article
Cite this article as:
Pagliero R.J., Pierini A.B., Brun R. and Mazzieri M.R., Design, Synthesis and 3-D Characterization of 1-Benzenesulfonyl-1,2,3,4- Tetrahydroquinolines as Lead Scaffold for Antiparasitic Drug, Letters in Drug Design & Discovery 2010; 7 (6) . https://dx.doi.org/10.2174/157018010791306614
DOI https://dx.doi.org/10.2174/157018010791306614 |
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
-
Disease Progression in Children with Vertically-Acquired HIV Infection in Sub-Saharan Africa: Reviewing the Need for HIV Treatment
Current HIV Research Calix[n]arenes as Goldmines for the Development of Chemical Entities of Pharmaceutical Interest
Current Pharmaceutical Design Targeting the Methyl Erythritol Phosphate (MEP) Pathway for Novel Antimalarial, Antibacterial and Herbicidal Drug Discovery: Inhibition of 1-Deoxy-D-Xylulose-5-Phosphate Reductoisomerase (DXR) Enzyme
Current Pharmaceutical Design Association of N-Acetyltransferase-2 Genotypes and Anti-Tuberculosis Induced Liver Injury: First Case-Controlled Study from Iran
Current Drug Safety Can Mandated BCG Vaccine Promote herd Immunity against Novel Coronavirus? A Potential Solution at Hand to Tackle Covid-19 Pandemic
Current Immunology Reviews (Discontinued) Anti-Infective Protective Properties of S100 Calgranulins
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Genetics and Vaccines in the Era of Personalized Medicine
Current Genomics Nanoembedded Microparticles for Stabilization and Delivery of Drug-Loaded Nanoparticles
Current Pharmaceutical Design Drug Metabolizing Enzymes and Transporters mRNA in Peripheral Blood Mononuclear Cells of Healthy Subjects: Biological Variations and Importance of Preanalytical Steps
Current Drug Metabolism Diagnostic Accuracy of Monocyte Chemotactic Protein (MCP)-2 as Biomarker in Response to PE35/PPE68 Proteins: A Promising Diagnostic Method for the Discrimination of Active and Latent Tuberculosis
Protein & Peptide Letters A New Era of Pulmonary Delivery of Nano-antimicrobial Therapeutics to Treat Chronic Pulmonary Infections
Current Pharmaceutical Design Editorial [ The Medicinal Chemistry of Anti-Infectious Agents Guest Editor: Concepcion Gonzalez-Bello ]
Current Topics in Medicinal Chemistry The Role of Universal Stress Proteins in Bacterial Infections
Current Medicinal Chemistry Hypocholesterolemia
Current Vascular Pharmacology Study of the Scientific Production on Leishmaniasis in Latin America
Recent Patents on Anti-Infective Drug Discovery Challenges and Opportunities of Nanotechnological based Approach for the Treatment of Tuberculosis
Current Pharmaceutical Design Key Amino Acids of Arabidopsis VKOR in the Activity of Phylloquinone Reduction and Disulfide Bond Formation
Protein & Peptide Letters Drug-Induced Hypokalaemia
Current Drug Safety Increased Production of Recombinant O-Phospho-L-Serine Sulfhydrylase from the Hyperthermophilic Archaeon Aeropyrum pernix K1 Using Escherichia coli
Current Biotechnology Platelets as Potential Immunomodulators: Is There a Role for Platelet Toll-Like Receptors?
Current Immunology Reviews (Discontinued)