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Research article
Rakesh Kumar Marwaha
Maharshi Dayanand University Rohtak
Corresponding Author
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Background : Looking at the extensive biological potential of thiazolidine-2,4-dione (TZD) moiety, a new series of thiazolidine-2,4-dione analogues was synthesized. Different spectral techniques ( 1 H-NMR, IR, MS etc.) were used to confirm the chemical structures of the synthesized analogues. These synthesized compounds were screened for their antioxidant and antimicrobial potential.
Results and discussion : The antimicrobial screening was carried out against selected strains of fungi and bacteria using serial tube dilution method. The antioxidant potential was assessed using stable 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging method. Further, the interaction between synthesized thiazolidine-2,4-dione compounds and DNA gyrase was explored using molecular docking studies. Various ADME parameters were also studied to evaluate the drug likeness of the synthesized compounds.
Conclusion: In antimicrobial evaluation, the compounds 4 , 9 , 11 , 12, 13 , 15 and 16 displayed promising activity against selected strains of microbes. Antioxidant evaluation found compound 6 having IC 50 = 9.18 μg/mL to be the most potent compound in the series. The molecular docking study revealed compounds 4 ( dock score = -4.73) and 7 (dock score = -4.61) with decent docking score, possess good interaction inside the ATP binding pocket of DNA gyrase and therefore can be used as lead structure for further optimizing into potent antimicrobial molecule.
Keywords
Thiazolidin-2,4-dione, Synthesis, Antimicrobial, Antioxidant, Characterization
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CURRENT STATUS: Published
View the published article at BMC Chemistry.
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Posted 15 Mar, 2020
No community comments so far
Editorial decision: Accept
On 16 Mar, 2020
Review #2 received
Received 14 Mar, 2020
Reviewers invited
Invitations sent on 11 Mar, 2020
Reviewer #1 agreed
On 11 Mar, 2020
Reviewer #2 agreed
On 11 Mar, 2020
Review #1 received
Received 11 Mar, 2020
Editor assigned
On 09 Mar, 2020
Submission checks complete
On 08 Mar, 2020
Editor invited
On 08 Mar, 2020
No comments provided
Editorial decision: Minor revision
On 27 Feb, 2020
Review #2 received
Received 25 Feb, 2020
Reviewer #1 agreed
On 24 Feb, 2020
Reviewer #2 agreed
On 24 Feb, 2020
Review #1 received
Received 24 Feb, 2020
Reviewers invited
Invitations sent on 24 Feb, 2020
Editor assigned
On 21 Feb, 2020
Submission checks complete
On 20 Feb, 2020
Editor invited
On 20 Feb, 2020
No comments provided
Review #1 received
Received 17 Feb, 2020
Editorial decision: Major revision
On 17 Feb, 2020
Reviewer #3 agreed
On 02 Feb, 2020
Review #3 received
Received 02 Feb, 2020
Review #2 received
Received 02 Feb, 2020
Reviewers invited
Invitations sent on 29 Jan, 2020
Reviewer #1 agreed
On 29 Jan, 2020
Reviewer #2 agreed
On 29 Jan, 2020
Editor assigned
On 21 Jan, 2020
Submission checks complete
On 20 Jan, 2020
Editor invited
On 20 Jan, 2020
First submitted
On 16 Jan, 2020
Metrics
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PDF Downloads: ...
HTML Views: ...
Subject Areas
Medicinal Chemistry
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See the published version of this preprint at BMC Chemistry.
This is a preprint, a preliminary version of a manuscript that has not completed peer review at a journal. Research Square does not conduct peer review prior to posting preprints. The posting of a preprint on this server should not be interpreted as an endorsement of its validity or suitability for dissemination as established information or for guiding clinical practice.
Learn more about In Review
Research article
Rakesh Kumar Marwaha
Maharshi Dayanand University Rohtak
Corresponding Author
Badges
Prescreen
This manuscript passed our Prescreen assessment
Complete author information
Appropriate declaration statements
Potential risks to human health
Prescreen
Peer Review Timeline
CURRENT STATUS: Published
View the published article at BMC Chemistry.
Version 3
Posted 15 Mar, 2020
No community comments so far
Editorial decision: Accept
On 16 Mar, 2020
Review #2 received
Received 14 Mar, 2020
Reviewers invited
Invitations sent on 11 Mar, 2020
Reviewer #1 agreed
On 11 Mar, 2020
Reviewer #2 agreed
On 11 Mar, 2020
Review #1 received
Received 11 Mar, 2020
Editor assigned
On 09 Mar, 2020
Submission checks complete
On 08 Mar, 2020
Editor invited
On 08 Mar, 2020
No comments provided
Editorial decision: Minor revision
On 27 Feb, 2020
Review #2 received
Received 25 Feb, 2020
Reviewer #1 agreed
On 24 Feb, 2020
Reviewer #2 agreed
On 24 Feb, 2020
Review #1 received
Received 24 Feb, 2020
Reviewers invited
Invitations sent on 24 Feb, 2020
Editor assigned
On 21 Feb, 2020
Submission checks complete
On 20 Feb, 2020
Editor invited
On 20 Feb, 2020
No comments provided
Review #1 received
Received 17 Feb, 2020
Editorial decision: Major revision
On 17 Feb, 2020
Reviewer #3 agreed
On 02 Feb, 2020
Review #3 received
Received 02 Feb, 2020
Review #2 received
Received 02 Feb, 2020
Reviewers invited
Invitations sent on 29 Jan, 2020
Reviewer #1 agreed
On 29 Jan, 2020
Reviewer #2 agreed
On 29 Jan, 2020
Editor assigned
On 21 Jan, 2020
Submission checks complete
On 20 Jan, 2020
Editor invited
On 20 Jan, 2020
First submitted
On 16 Jan, 2020
Metrics
Comments: 0
PDF Downloads: ...
HTML Views: ...
Subject Areas
Medicinal Chemistry
License:
This work is licensed under a CC BY 4.0 License. Read Full License
View the published article at BMC Chemistry.
Background : Looking at the extensive biological potential of thiazolidine-2,4-dione (TZD) moiety, a new series of thiazolidine-2,4-dione analogues was synthesized. Different spectral techniques ( 1 H-NMR, IR, MS etc.) were used to confirm the chemical structures of the synthesized analogues. These synthesized compounds were screened for their antioxidant and antimicrobial potential.
Results and discussion : The antimicrobial screening was carried out against selected strains of fungi and bacteria using serial tube dilution method. The antioxidant potential was assessed using stable 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging method. Further, the interaction between synthesized thiazolidine-2,4-dione compounds and DNA gyrase was explored using molecular docking studies. Various ADME parameters were also studied to evaluate the drug likeness of the synthesized compounds.
Conclusion: In antimicrobial evaluation, the compounds 4 , 9 , 11 , 12, 13 , 15 and 16 displayed promising activity against selected strains of microbes. Antioxidant evaluation found compound 6 having IC 50 = 9.18 μg/mL to be the most potent compound in the series. The molecular docking study revealed compounds 4 ( dock score = -4.73) and 7 (dock score = -4.61) with decent docking score, possess good interaction inside the ATP binding pocket of DNA gyrase and therefore can be used as lead structure for further optimizing into potent antimicrobial molecule.
Figure 1
Figure 2
Figure 3
Figure 4
Figure 5
Figure 6
Figure 7
Figure 8
Figure 9
This is a list of supplementary files associated with this preprint. Click to download.
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