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Research Journal of Pharmacy and Technology
Year : 2018, Volume : 11, Issue : 12
First page : ( 5611) Last page : ( 5622)
Print ISSN : 0974-3618. Online ISSN : 0974-360X.
Article DOI : 10.5958/0974-360X.2018.01019.3

Synthesis, Antimicrobial Evaluation and Molecular Docking Studies of Novel Oxazolidinone-Thiophene Chalcone Hybrid Derivatives

Panigrahi Naresh1,2,*, Ganguly Swastika2, Panda Jagadeesh3

1GITAM Institute of Pharmacy, GITAM (Deemed to be University), Rushikonda, Visakhapatnam-530 045

2Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology, Mesra, Ranchi-835 215

3Raghu College of Pharmacy, Dakamarri, Bheemunipatnam, Visakhapatnam, 531 162, India

*Corresponding Author E-mail: naresh.panigrahi@gitam.edu

Online published on 18 May, 2019.

Abstract

In the present study, in order to synthesize broad-spectrum antibacterial agents, we coupled both the oxazolidinone and novel thiophene chalcone derivatives by using Buchwald's protocol under ultrasound irradiation. All the newly synthesized 20 oxazolidinone-thiophene chalcone hybrid compounds were characterized by IR, 1HNMR and Mass spectral analysis and evaluated for in vitro antibacterial and antifungal activities. Antibacterial and antifungal activities were tested using the serial dilution method. The test compounds 7e to 7g exhibited very high activities at 3.125 μg/ml when compared to the standard drug linezolid and were as other compounds showed moderate to weak activities. In case of antifungal activities, the test compounds 7e to 7g, 7i, 7j, and 7m to 7o exhibited moderate activities compared to the standard fluconazole, whereas the rest of the compounds showed weak activities against tested fungal strains. The binding mode analysis of the test compounds 7e to 7g were investigated by the docking studies using Glide 6.6., inside the active site of peptidyl transferase center of E.coli ribosome (PDB ID: 2AW4), revealed that the experimental results were comparable to that of co-crystallized ligand linezolid.

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Keywords

Ultrasound (US) irradiation, lithium hydroxide monohydrate (LiOH·H2O), aryl aldehydes, potassium hydroxide (KOH), docking and ADME studies.

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