Title:Synthesis and Antibacterial/Antitubercular/Antioxidant Activities of Compounds Containing Fluoroquinolone Ring Linked to a 4-thiazolidinone Moiety
Volume: 15
Issue: 10
Author(s): Tejeswara Rao Allaka, Naresh Kumar Katari, Venkanna Banothu, Srinubabu Maddela, Manojit Pal*Jaya Shree Anireddy*
Affiliation:
- Dr. Reddy`s Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad,India
- Centre for Chemical Sciences and Technology, Institute of Science & Technology, Jawaharlal Nehru Technological University Hyderabad, Kukatpally, Hyderabad, Telangana,India
Keywords:
Fluoroquinolone, 4-thiazolidinone, antitubercular, antioxidant, antifungal, mycobacterium genus.
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.