Abstract
Twenty-two 4-aryl/alkyl-1-(diphenylacetyl)thiosemicarbazides were synthesized and their in vitro antibacterial potency was evaluated. 4-(4-Chlorophenyl)-1-diphenylacetylthiosemicarbazide showed comparable activity to control antibacterial ampicillin against Gram-positive species with MICs range 3.91-15.63 µg/mL. The compound was also tested for its cytotoxicity against L929 cell line using the MTT assay technique. The results of antibacterial activity and toxicity test indicated that it display antibacterial activity at non-cytotoxic concentrations. Finally, some structural and electronic parameters have been determined in hope to get insight into different biological activity of closely related isomers.
Keywords: Antibacterial activity, Structure-activity relationship (SAR) studies, Thiosemicarbazide derivatives.
Letters in Drug Design & Discovery
Title:Antibacterial Activity and Structure-Activity Relationship Studies of 4- aryl/alkyl-1-(diphenylacetyl)thiosemicarbazides
Volume: 10 Issue: 8
Author(s): Edyta Kusmierz, Agata Siwek, Urszula Kosikowska, Anna Malm, Joanna Stefanska, Katarzyna Dzitko and Monika Wujec
Affiliation:
Keywords: Antibacterial activity, Structure-activity relationship (SAR) studies, Thiosemicarbazide derivatives.
Abstract: Twenty-two 4-aryl/alkyl-1-(diphenylacetyl)thiosemicarbazides were synthesized and their in vitro antibacterial potency was evaluated. 4-(4-Chlorophenyl)-1-diphenylacetylthiosemicarbazide showed comparable activity to control antibacterial ampicillin against Gram-positive species with MICs range 3.91-15.63 µg/mL. The compound was also tested for its cytotoxicity against L929 cell line using the MTT assay technique. The results of antibacterial activity and toxicity test indicated that it display antibacterial activity at non-cytotoxic concentrations. Finally, some structural and electronic parameters have been determined in hope to get insight into different biological activity of closely related isomers.
Export Options
About this article
Cite this article as:
Kusmierz Edyta, Siwek Agata, Kosikowska Urszula, Malm Anna, Stefanska Joanna, Dzitko Katarzyna and Wujec Monika, Antibacterial Activity and Structure-Activity Relationship Studies of 4- aryl/alkyl-1-(diphenylacetyl)thiosemicarbazides, Letters in Drug Design & Discovery 2013; 10 (8) . https://dx.doi.org/10.2174/15701808113100890028
DOI https://dx.doi.org/10.2174/15701808113100890028 |
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
-
Estimation of Affinity of HLA-A*0201 Restricted CTL Epitope Based on the SCORE Function
Protein & Peptide Letters Seco-Tetracyclic and Seco-Pentacyclic Triterpenoids from Nature: Phytochemistry, Biological Activity: A Review
Mini-Reviews in Organic Chemistry Recognition and Function of HumanγδT Cells: Application for Tumor Immunotherapy
Current Immunology Reviews (Discontinued) Developing Country Applications of Molecular Farming: Case Studies in South Africa and Argentina
Current Pharmaceutical Design The Synthetic Potential and Chemical Aspects of the Gewald Reaction: Application in the Preparation of 2-Aminothiophenes and Related Heterocycles
Current Organic Synthesis CAPi: Computational Model for Apicoplast Inhibitors Prediction Against Plasmodium Parasite
Current Computer-Aided Drug Design Role of FoxP3<sup>+</sup> Treg Cells Mediating Immune Suppression in Leprosy
Current Immunology Reviews (Discontinued) Imidazole and Pyrazole: Privileged Scaffolds for Anti-Infective Activity
Mini-Reviews in Organic Chemistry The Use of Biologic Therapies in the Treatment of Rheumatoid Arthritis
Current Pharmaceutical Biotechnology Dietary Nitrite in Nitric Oxide Biology: A Redox Interplay with Implications for Pathophysiology and Therapeutics
Current Drug Targets Designed Multiple Ligands: Basic Research vs Clinical Outcomes
Current Medicinal Chemistry EHDA Spraying: A Multi-Material Nano-Engineering Route
Current Pharmaceutical Design Mesenchymal Stem Cells as a Treatment Strategy for Coronavirus Disease 2019 (COVID-19): Need for Authority Regulations and Clinical Guidelines
Current Stem Cell Research & Therapy The Epidemiology and Health Effects of Tobacco Use
Current Pediatric Reviews Uveitis in Horses, Rats and Man: What Do We Learn from Our Pets?
Current Immunology Reviews (Discontinued) Perspectives and Prospects on mRNA Vaccine Development for COVID-19
Current Medicinal Chemistry Recent Developments of Thalidomide Derivatives Possessing Anti-Inflammatory Activity
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry The Long Pentraxin PTX3, a Soluble Pattern Recognition Receptor Involved in Innate Immunity,Inflammation and Female Fertility
Current Immunology Reviews (Discontinued) Can Probiotics Cure Inflammatory Bowel Diseases?
Current Pharmaceutical Design Triazole-linked Chalcone and Flavone Hybrid Compounds Based on AZT Exhibiting In Vitro Anti-Cancer Activity
Letters in Drug Design & Discovery