Submit Manuscript  

Article Details


Design, Synthesis, Docking and Biological Evaluation of Novel 4-hydroxy Coumarin Derivatives

Author(s):

N. Ramalakshmi, S.R. Chitra*, P. Manimegalai and S. Arunkumar   Pages 1 - 13 ( 13 )

Abstract:


Background: Hospital acquired (HA) infections are caused due to E. coliwhich is resistant to multiple drugs particularly to fluroquinolone class of drugs. Urinary tract infections (UTI) affects people in the community and in hospitals. 150 million people per annum are suffering from UTI worldwide.

Methods: In this present study we designed 36 novel coumarin derivatives, also we predicted pharmacokinetic and toxicity parameters. Docking studies were also carriedand all the compounds were evaluated for antibacterial activity againstresistant quinolone E. coli strain ATCC 25922. It was interesting to note thatthe introduction of electron withdrawing group on the aromatic ringresulted in compounds with increased antibacterial activity which is observed in compound 6 (with4-nitro substitution), compound 23(chloro) and compound 30(chloro, nitro).

Results: From the MIC results, was observed that compounds 6, 23 and 30 showed higher activity with 0.5µg/ml, 0. 12 µg/ml, 0.5 µg/mlrespectively. Docking studies were performed with the activesite of DNA gyrase (PDB ID: 4CKK ).The maximum binding energy was found to be -10.7Kcal/mol. Conclusion: From the study it was found that 3 compounds were potentially active against quinolone resistant E. coli strains. This study can be further extended for in vivo evaluation.

Keywords:

DNA Gyrase, Antibacterial, coumarin, Azetidinone, Docking, Insilico studies

Affiliation:

Department of Pharmaceutical Chemistry, C.L. BaidMetha College of Pharmacy, Thoraipakkam, Chennai-97, Tamil Nadu, Department of Pharmaceutical Chemistry, C.L. BaidMetha College of Pharmacy, Thoraipakkam, Chennai-97, Tamil Nadu, College of Pharmaceutical Sciences, Gulf Medical University, Ajmaan, College of Pharmaceutical Sciences, Gulf Medical University, Ajmaan



Read Full-Text article