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Research Article
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The synthesis of novel 1,4-naphthoquinone derivatives has attracted prominent interest in the field of medicinal chemistry since these compounds exhibit potent pharmacological activity as antibacterial, antioxidant, antifungal, and anticancer. Herein, a series of novel 1,4-naphthoquinone derivatives 4-7, 8a-c, and 9a-d containing heterocyclic moieties were synthesized in good yields and characterized by spectral and elemental analyses. All the new synthesized compounds were subjected to in-vitro antimicrobial testing against gram-positive, gram-negative, and fungal strains by calculating the average of the zone of inhibition. The antimicrobial results showed that compounds 8b, 9b, and 9c displayed the highest efficacy against both bacterial and fungal strains. Further studies have been conducted to estimate the antioxidant activity of the compounds using DPPH scavenging assay. The obtained results revealed that compounds 9d, 9a, 9b, 8c, and 6 exhibited the highest radical scavenging activity. Docking studies of the most active antimicrobial compounds within GLN- 6-P, recorded good scores with several binding interactions with the active site.
Keywords
Heterocycles, 1,4-naphthoquinone, antimicrobial, antioxidant, molecular docking
Figure 1
Figure 2
Figure 3
Figure 4
Figure 5
This is a list of supplementary files associated with this preprint. Click to download.
- Scheme01.png
Scheme 1 Synthesis of compounds 3-6
- Scheme02.png
Scheme 2 Synthesis of compounds 7 and 8a-c
- Scheme03.png
Scheme 3 Synthesis of compounds 9a-d
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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.
Research Article
Badges
Prescreen
This manuscript passed our Prescreen assessment
Complete author information
Appropriate declaration statements
Potential risks to human health
Prescreen
History
CURRENT STATUS: Posted
Version 1
Posted 06 Mar, 2021
No community comments so far
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
The synthesis of novel 1,4-naphthoquinone derivatives has attracted prominent interest in the field of medicinal chemistry since these compounds exhibit potent pharmacological activity as antibacterial, antioxidant, antifungal, and anticancer. Herein, a series of novel 1,4-naphthoquinone derivatives 4-7, 8a-c, and 9a-d containing heterocyclic moieties were synthesized in good yields and characterized by spectral and elemental analyses. All the new synthesized compounds were subjected to in-vitro antimicrobial testing against gram-positive, gram-negative, and fungal strains by calculating the average of the zone of inhibition. The antimicrobial results showed that compounds 8b, 9b, and 9c displayed the highest efficacy against both bacterial and fungal strains. Further studies have been conducted to estimate the antioxidant activity of the compounds using DPPH scavenging assay. The obtained results revealed that compounds 9d, 9a, 9b, 8c, and 6 exhibited the highest radical scavenging activity. Docking studies of the most active antimicrobial compounds within GLN- 6-P, recorded good scores with several binding interactions with the active site.
Figure 1
Figure 2
Figure 3
Figure 4
Figure 5
This is a list of supplementary files associated with this preprint. Click to download.
- Scheme01.png
Scheme 1 Synthesis of compounds 3-6
- Scheme02.png
Scheme 2 Synthesis of compounds 7 and 8a-c
- Scheme03.png
Scheme 3 Synthesis of compounds 9a-d
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