Tehran University of Medical Sciences

Science Communicator Platform

Stay connected! Follow us on X network (Twitter):
Share this content! On (X network) By
Biology-Oriented Drug Synthesis (Biods) Approach Towards Synthesis of Ciprofloxacin-Dithiocarbamate Hybrids and Their Antibacterial Potential Both in Vitro and in Silico Publisher Pubmed



Esfahani EN1 ; Mohammadikhanaposhtani M2 ; Rezaei Z3 ; Valizadeh Y3 ; Rajabnia R4 ; Bagheri M5 ; Bandarian F1 ; Faramarzi MA6 ; Samadi N7 ; Amini MR8 ; Mahdavi M8 ; Larijani B8
Authors
Show Affiliations
Authors Affiliations
  1. 1. Diabetes Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran
  2. 2. Cellular and Molecular Biology Research Center, Health Research Institute, Babol University of Medical Sciences, Babol, Iran
  3. 3. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
  4. 4. Infectious Diseases and Tropical Medicine Research Center, Babol University of Medical Sciences, Babol, Iran
  5. 5. Infectious Diseases Research Center, Babol University of Medical Sciences, Babol, Iran
  6. 6. Department of Pharmaceutical Biotechnology, Faculty of Pharmacy and Biotechnology Research Center, Tehran University of Medical Sciences, Tehran, Iran
  7. 7. Department of Drug and Food Control, Faculty of Pharmacy and Pharmaceutical Quality Assurance Research Center, Tehran University of Medical Sciences, Tehran, Iran
  8. 8. Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran

Source: Chemistry and Biodiversity Published:2018


Abstract

A novel series of ciprofloxacin-dithiocarbamate hybrids 7a – 7l were designed, synthesized, and evaluated against Gram-positive and Gram-negative bacteria. A significant part of the title compounds showed considerable antibacterial activity against Gram-positive species. The most potent compound against Gram-positive bacteria was 2-chloro derivative 7h and the most potent derivative against Gram-negative bacteria was 3-chloro compound 7i. In vitro antibacterial evaluation of compound 7h against clinically isolated bacteria methicillin-resistant Staphylococcus aureus (MRSA) and methicillin-sensitive Staphylococcus aureus (MSSA) showed that this compound acted better than ciprofloxacin against the latter bacteria. Docking study of compound 7h in the active site of S. aureus DNA gyrase revealed that this ciprofloxacin-dithiocarbamate derivative interacted with the main components of the active site of the enzyme. © 2018 Wiley-VHCA AG, Zurich, Switzerland
Related Docs
View other Related Docs
1. New Biscoumarin Derivatives As Potent Α-Glucosidase Inhibitors: Synthesis, Biological Evaluation, Kinetic Analysis, and Docking Study, Polycyclic Aromatic Compounds (2020)
2. Design, Synthesis, in Vitro Cytotoxic Activity Evaluation, and Study of Apoptosis Inducing Effect of New Styrylimidazo[1,2-A]Pyridines As Potent Anti-Breast Cancer Agents, Anti-Cancer Agents in Medicinal Chemistry (2019)
3. Novel Tetrahydrocarbazole Benzyl Pyridine Hybrids As Potent and Selective Butryl Cholinesterase Inhibitors With Neuroprotective and Β-Secretase Inhibition Activities, European Journal of Medicinal Chemistry (2018)
4. Design, Synthesis, Molecular Docking Study, and Antibacterial Evaluation of Some New Fluoroquinolone Analogues Bearing a Quinazolinone Moiety, DARU# Journal of Pharmaceutical Sciences (2020)
5. Synthesis and Biological Activity of Some Benzochromenoquinolinones: Tacrine Analogs As Potent Anti-Alzheimer's Agents, Chemistry and Biodiversity (2019)
6. Design, Synthesis, and Cholinesterase Inhibition Assay of Coumarin-3-Carboxamide-N-Morpholine Hybrids As New Anti-Alzheimer Agents, Chemistry and Biodiversity (2019)
7. Design and Synthesis of Multi-Target Directed 1,2,3-Triazole-Dimethylaminoacryloyl-Chromenone Derivatives With Potential Use in Alzheimer's Disease, BMC Chemistry (2020)
8. Recent Developments in the Design and Synthesis of Benzylpyridinium Salts: Mimicking Donepezil Hydrochloride in the Treatment of Alzheimer’S Disease, Frontiers in Chemistry (2022)
Experts (# of related papers)
View all Related Experts
Mohammad Mahdavi (12)
Bagher Larijani (7)
Other Related Docs
9. Novel N-Benzylpyridinium Moiety Linked to Arylisoxazole Derivatives As Selective Butyrylcholinesterase Inhibitors: Synthesis, Biological Evaluation, and Docking Study, Bioorganic Chemistry (2019)
10. New Benzyl Pyridinium Derivatives Bearing 2,4-Dioxochroman Moiety As Potent Agents for Treatment of Alzheimer's Disease: Design, Synthesis, Biological Evaluation, and Docking Study, Bioorganic Chemistry (2019)
11. Pyrano[3,2-C]Quinoline Derivatives As New Class of Α-Glucosidase Inhibitors to Treat Type 2 Diabetes: Synthesis, in Vitro Biological Evaluation and Kinetic Study, Medicinal Chemistry (2019)
12. Design, Synthesis, and Biological Evaluation of Selective and Potent Carbazole-Based Butyrylcholinesterase Inhibitors, Bioorganic and Medicinal Chemistry (2018)
13. Anticholinesterase Activity of Cinnamic Acids Derivatives: In Vitro, in Vivo Biological Evaluation, and Docking Study, Letters in Drug Design and Discovery (2020)
14. Design, Synthesis and Cytotoxicity of Novel Coumarin-1,2,3-Triazole-1,2,4-Oxadiazole Hybrids As Potent Anti-Breast Cancer Agents, Letters in Drug Design and Discovery (2019)