Abstract
This paper describes the synthesis and in vitro biological activities of imidazolidine and hexahydropyrimidine derivatives against bacteria (Escherichia coli, Staphylococcus aureus and Mycobacterium tuberculosis) and Leishmania protozoa. Out of sixteen heterocyclic derivatives tested, none were cytotoxic against mammalian cells. The compounds showed significant bacterial effects and leishmanicidal activity. Compounds 4a and 4c were active against S. aureus and E. coli, respectively. Compounds 3a-3f, 4h and 4i presented promising results against M. tuberculosis, with MIC values ranging from 12.5 to 25.0 μg/mL, comparable to the “first and second line” drugs used to treat tuberculosis. Compounds 4a, 4c and 4e were active against L major. Three of them were structurally characterized by single-crystal X-ray diffraction.
Keywords: Synthesis, Cytotoxicity, Antibacterial, Antileishmanial, Biological Activities, Imidazolidine, Hexahydropyrimidine Derivatives, X-ray crystallography, Mycobacterium tuberculosis, heterocyclic compounds, E. coli
Medicinal Chemistry
Title:Synthesis, Cytotoxicity, Antibacterial and Antileishmanial Activities of Imidazolidine and Hexahydropyrimidine Derivatives
Volume: 9 Issue: 3
Author(s): Gustavo S. G. de Carvalho, Rafael M. P. Dias, Fernando R. Pavan, Clarice Q. F. Leite, Vania L. Silva, Claudio G. Diniz, Daniela T. S. de Paula, Elaine S. Coimbra, Pascal Retailleau and Adilson D. da Silva
Affiliation:
Keywords: Synthesis, Cytotoxicity, Antibacterial, Antileishmanial, Biological Activities, Imidazolidine, Hexahydropyrimidine Derivatives, X-ray crystallography, Mycobacterium tuberculosis, heterocyclic compounds, E. coli
Abstract: This paper describes the synthesis and in vitro biological activities of imidazolidine and hexahydropyrimidine derivatives against bacteria (Escherichia coli, Staphylococcus aureus and Mycobacterium tuberculosis) and Leishmania protozoa. Out of sixteen heterocyclic derivatives tested, none were cytotoxic against mammalian cells. The compounds showed significant bacterial effects and leishmanicidal activity. Compounds 4a and 4c were active against S. aureus and E. coli, respectively. Compounds 3a-3f, 4h and 4i presented promising results against M. tuberculosis, with MIC values ranging from 12.5 to 25.0 μg/mL, comparable to the “first and second line” drugs used to treat tuberculosis. Compounds 4a, 4c and 4e were active against L major. Three of them were structurally characterized by single-crystal X-ray diffraction.
Export Options
About this article
Cite this article as:
S. G. de Carvalho Gustavo, M. P. Dias Rafael, R. Pavan Fernando, Q. F. Leite Clarice, L. Silva Vania, G. Diniz Claudio, T. S. de Paula Daniela, S. Coimbra Elaine, Retailleau Pascal and D. da Silva Adilson, Synthesis, Cytotoxicity, Antibacterial and Antileishmanial Activities of Imidazolidine and Hexahydropyrimidine Derivatives, Medicinal Chemistry 2013; 9 (3) . https://dx.doi.org/10.2174/1573406411309030005
DOI https://dx.doi.org/10.2174/1573406411309030005 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
Call for Papers in Thematic Issues
Carbohydrates in Computational and Medicinal Chemistry
Carbohydrates are the most essential organic molecules and are involved in the maintenance of various physiological and metabolic processes in living organisms. Carbohydrate-based compounds have come to the attention of researchers because of their significant contributions to biological functions, such as cell development and cell proliferation, connections between several cells, ...read more
Recent Advances in the Medicinal Chemistry of Cancer
Scope of the Thematic Issue: Correlation between structure and function is one of the important aspects of the success of anti-cancer compounds associated with their structure-activity interactions, physiology, biochemical, molecular, and genetic processes. Overcoming these obstacles is key to obtaining further insights into developments in rational drug design, bioorganic chemistry, ...read more
- 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
-
Nitric Oxide Production and Signaling in Inflammation
Current Drug Targets - Inflammation & Allergy Advancement in Vaccinology: New Era in Formulation Strategies
Current Drug Therapy Synthesis of Bicyclic Aryl Thiazolines with Selective Anti-Proliferative Effects on Human Cancer Cell Lines
Letters in Organic Chemistry Genomic and Genetic Approaches for the Identification of Antifungal Drug Targets
Infectious Disorders - Drug Targets EDITORIAL: Vaccinology in the 21st century
Current Topics in Medicinal Chemistry Benzothiazole: A Versatile and Multitargeted Pharmacophore in the Field of Medicinal Chemistry
Letters in Organic Chemistry Can Chest Computed Tomography Findings of Symptomatic COVID-19 Patients Upon Admission Indicate Disease Prognosis and Clinical Outcome?
Current Medical Imaging Arylamine N-Acetyltransferases in Mycobacteria
Current Drug Metabolism Genus Euonymus: Chemical and Pharmacological Perception
Mini-Reviews in Organic Chemistry Electrotransfer into Skeletal Muscle for Protein Expression
Current Gene Therapy Is Human Immunodeficiency Virus-Mediated Dementia an Autophagic Defect that Leads to Neurodegeneration?
CNS & Neurological Disorders - Drug Targets MIANN Models of Networks of Biochemical Reactions, Ecosystems, and U.S. Supreme Court with Balaban-Markov Indices
Current Bioinformatics The Effect of Chemotherapy/Radiotherapy on Cancerous Pattern Recognition by NK Cells
Current Medicinal Chemistry Cytokine Therapeutics for the Treatment of Sepsis: Why has Nothing Worked?
Current Pharmaceutical Design Synthesis and Cytotoxicity of Amino-Pyrazole Derivatives with Preliminary SAR
Letters in Drug Design & Discovery New Approaches to Drug-DNA Interactions Based on Graphical Representation and Numerical Characterization of DNA Sequences
Current Computer-Aided Drug Design Is uPAR the Centre of a Sensing System Involved in the Regulation of Inflammation?
Current Medicinal Chemistry - Anti-Inflammatory & Anti-Allergy Agents A Tour of Unsupervised Deep Learning for Medical Image Analysis
Current Medical Imaging Anti - TNF Therapy for Crohns Disease
Current Pharmaceutical Design Synthesis and Anti-Proliferative Evaluations of New Heterocyclic Derivatives Using 5,6,8,9-Tetrahydropyrazolo[5,1-b]quinazolin-7(3H)-one Derivatives Derived from Cyclohexa-1,4-dione
Anti-Cancer Agents in Medicinal Chemistry