Synthesis and Antibacterial/Antitubercular/Antioxidant Activities of Compounds Containing Fluoroquinolone Ring Linked to a 4-thiazolidinone Moiety

Author(s): Tejeswara Rao Allaka, Naresh Kumar Katari, Venkanna Banothu, Srinubabu Maddela, Manojit Pal*, Jaya Shree Anireddy*

Journal Name: Letters in Drug Design & Discovery

Volume 15 , Issue 10 , 2018

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Graphical Abstract:


Background: Tuberculosis (TB), a contagious airborne disease caused by pathogen Mycobacterium tuberculosis (M. tb) is the second leading cause of death world-wide among the transferable diseases. It is therefore necessary to devote continuing effort for the identification and development of New Chemical Entities (NCEs) as potential antimicrobial agents to address this serious health problem.

Methods: A series of new compounds containing fluoroquinolone ring linked to a 4-thiazolidinone moiety were synthesized and evaluated for their potential pharmacological properties. The ZnCl2 mediated construction of 4-thiazolidinone ring via the condensation/cyclization of Schiff bases with thioglycolic acid was used as a key step for the multi-step synthesis of this class of compounds.

Results: When tested for antibacterial, antifungal, antitubercular activities in vitro and antioxidant activities several of these compounds showed good activities. Two compounds showed activities against both gram-(+) and gram-(-) strains and Mycobacterium smegmatis H37Rv ATCC 27294 (MTB) with MIC 16.28 and 27.86 µM, respectively. They also showed free radical scavenging properties with IC50 values in the range 23-33 μM and are appeared to be promising.

Conclusion: Our study revealed that the molecular framework presented here could be a useful template for the identification of novel small molecules as promising antimicrobial / amtitubercular agents.

Keywords: Fluoroquinolone, 4-thiazolidinone, antitubercular, antioxidant, antifungal, mycobacterium genus.

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Article Details

Year: 2018
Published on: 29 December, 2017
Page: [1087 - 1094]
Pages: 8
DOI: 10.2174/1570180815666171229150032
Price: $65

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