Abstract
Thirteen α-aminophosphonate derivatives with artesunate were synthesized by introducing bioactive α-aminophosphonate combination with artesunate in this work. The reaction were easily carried out at normal pressure, low temperature and without any catalyst. Four strains of microbials, namely Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Candida albicans, were used for the evaluation of the antimicrobial activities of these target compounds. Experimental results indicated that most of the compounds had good inhibitory effects. Compound 7k showed obvious antimicrobial activities with the MICs of 64 μg/ml against Staphylococcus aureus and 32 μg/ml against Candida albicans. Furthermore, when combined with roxithromycin, the synthesized compounds showed overlapping enhanced activities and proved potential antimicrobial synergists of roxithromycin.
Keywords: Artesunate, α-aminophosphonate, Antimicrobial Activity, Synthesis.
Letters in Drug Design & Discovery
Title:Synthesis of Derivatives of Artesunate α-Aminophosphonate and Their Antimicrobial Activities
Volume: 12 Issue: 5
Author(s): Sheng He, Xilin Ouyang, Xiaochao Huang, Weisong Hu, Weilong Dai, Xiaoyan Tian, Yingming Pan, Shiwen Huang and Hengshan Wang
Affiliation:
Keywords: Artesunate, α-aminophosphonate, Antimicrobial Activity, Synthesis.
Abstract: Thirteen α-aminophosphonate derivatives with artesunate were synthesized by introducing bioactive α-aminophosphonate combination with artesunate in this work. The reaction were easily carried out at normal pressure, low temperature and without any catalyst. Four strains of microbials, namely Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Candida albicans, were used for the evaluation of the antimicrobial activities of these target compounds. Experimental results indicated that most of the compounds had good inhibitory effects. Compound 7k showed obvious antimicrobial activities with the MICs of 64 μg/ml against Staphylococcus aureus and 32 μg/ml against Candida albicans. Furthermore, when combined with roxithromycin, the synthesized compounds showed overlapping enhanced activities and proved potential antimicrobial synergists of roxithromycin.
Export Options
About this article
Cite this article as:
He Sheng, Ouyang Xilin, Huang Xiaochao, Hu Weisong, Dai Weilong, Tian Xiaoyan, Pan Yingming, Huang Shiwen and Wang Hengshan, Synthesis of Derivatives of Artesunate α-Aminophosphonate and Their Antimicrobial Activities, Letters in Drug Design & Discovery 2015; 12 (5) . https://dx.doi.org/10.2174/1570180812666141125004502
DOI https://dx.doi.org/10.2174/1570180812666141125004502 |
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
-
Recent Trends in the Pharmacological Activity of Isoprenyl Phenolics
Current Medicinal Chemistry Anal Cancer: Focus on HIV-Positive Patients in the HAART Era
Current HIV Research Fibroblast Growth Factors/Fibroblast Growth Factor Receptors as Targets for the Development of Anti-Angiogenesis Strategies
Current Pharmaceutical Design Transport Mechanism-Based Drug Molecular Design: Novel Camptothecin Analogues to Circumvent ABCG2-associated Drug Resistance of Human Tumor Cells
Current Pharmaceutical Design Kinase Inhibitors Targeting Anti-angiogenesis as Anti-cancer Therapies
Current Angiogenesis (Discontinued) Effects of Antiretroviral Therapy on Immunity in Patients Infected with HIV
Current Pharmaceutical Design Cullin-RING Ligases as Attractive Anti-cancer Targets
Current Pharmaceutical Design Mesenchymal Stem Cells: Key Actors in Tumor Niche
Current Stem Cell Research & Therapy Design, Synthesis and Biological Evaluation of Hybrid Molecules Containing Conjugated Styryl Ketone and α-Bromoacryloyl Moieties
Letters in Drug Design & Discovery DNA Double Strand Break Repair - Related Synthetic Lethality
Current Medicinal Chemistry Undermining Tumor Angiogenesis by Gene Therapy: An Emerging Field
Current Gene Therapy Integrins: Regulators of Tissue Function and Cancer Progression
Current Pharmaceutical Design Signal transduction in Acute Myeloid Leukemia – Implications for Novel Therapeutic Concepts.
Current Cancer Drug Targets Astatine Radiopharmaceuticals: Prospects and Problems
Current Radiopharmaceuticals The Effect of Lycopene on the PI3K/Akt Signalling Pathway in Prostate Cancer
Anti-Cancer Agents in Medicinal Chemistry QSAR study on N- (Aryl)-4-(Azolylethyl) Thiazole-5-Carboxamides: Novel Potent Inhibitors of VEGF Receptors I and II
Medicinal Chemistry Developments in the Application of 1,2,3-Triazoles in Cancer Treatment
Recent Patents on Anti-Cancer Drug Discovery Giant Cell Arteritis – A Series of Cases and Review of Literature
Current Rheumatology Reviews Targeted Drugs and Nanomedicine: Present and Future
Current Pharmaceutical Design Clinical Development of MET Targeted Therapy For Human Cancer
Current Cancer Therapy Reviews