Abstract: (1838 Views)
Background and Objective: Fluoroquinolones are an important group of antimicrobial agents that are used widely in the treatment of various infectious diseases. Because resistance to antimicrobial drugs is widespread, new antimicrobial and understanding of their mechanisms of action are vital. The mechanism of action of these drugs is mediated by inhibition of DNA gyrase, topoisomerase II, IV. Here, substituent on the 7-position would play a key role. The aim of this study was the synthesis and evaluation of antimicrobial effects of new derivatives of Gatifloxacin, derived from substitution on the 7-position of quinilone.
Materials and Methods: In this laboratoty study, a series of gatifloxacin derivatives (2-oxo and 2- oxyimino-2-phenyl ethyl derivatives) were synthesized and evaluated for in-vitro antibacterial activity against a panel of standard gram positive and gram negative bacteria, using conventional agar dilution method.
Results: Among the tested compounds, in comparison with Ciprofloxacin, Gatifloxacin and other synthesized compounds, some analogues of Gatifloxacin (2e and 4e) was the most potent against gram positive bacteria. These compounds had no significant antibacterial activity against gram negative bacteria.
Conclusion: The presence of 2,4-dichloro on benzene ring could increase the antibacterial activity of those compounds. Totally, in comparison with Ciprofloxacin and Gatifloxacin, the tested compounds had the most potent antibacterial activity against gram positive bacteria. All compounds showed no significant activity against gram-negative bacteria.
Key words: Florouquinolones, Gatifloxacin, Antibacterial activity
Funding: This research was funded by Kerman University of Medical Sciences.
Conflict of Interest: None declared.
Athical Approval: The Ethical Committee of Kerman University of Medical Sciences approved the study.
How to cite this article: Moshafi MH, Mohammadhosseini N, Saffari F, Arjomand Sh, Farmanara B, A. Foroumadi. Synthesis and in vitro Antibacterial Activity of 2-oxo and 2- Oxyimino-2-Phenyl Ethyl Gatifloxacin Derivatives. J Rafsanjan Univ Med Scie 2013; 12(6): 425-36 . [Farsi]
Type of Study:
Research |
Subject:
Biochemistry Received: 2020/05/9 | Accepted: 2020/05/9 | Published: 2020/05/9