Biology‐Oriented Drug Synthesis (BIODS) Approach towards Synthesis of Ciprofloxacin‐Dithiocarbamate Hybrids and Their Antibacterial Potential both in Vitro and in Silico. Issue 10 (24th September 2018)

• Record Type: Journal Article
• Authors: Esfahani, Ensieh Nasli; Mohammadi‐Khanaposhtani, Maryam; Rezaei, Zahra; Valizadeh, Yosef; Rajabnia, Ramazan; Bagheri, Meghdad; Bandarian, Fatemeh; Faramarzi, Mohammad Ali; Samadi, Nasrin; Amini, Mohammad Reza; Mahdavi, Mohammad; Larijani, Bagher
• Is Part Of: Chemistry & biodiversity. Volume 15:Issue 10(2018)
• Page Start: n/a
• Page End: n/a
• Publication Date: 2018-09-24
• Subjects: ciprofloxacin -- dithiocarbamate -- docking study -- antibacterial activity -- BIODS; Biochemistry -- Periodicals; Molecular biology -- Periodicals; Biodiversity -- Periodicals; 572
• DOI: 10.1002/cbdv.201800273
• Languages: English
• ISSNs: 1612-1872

Abstract

Abstract : A novel series of ciprofloxacin‐dithiocarbamate hybrids7a – 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 derivative7h and the most potent derivative against Gram‐negative bacteria was 3‐chloro compound7i . In vitro antibacterial evaluation of compound7h 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 compound7h 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. Abstract :