Expeditious synthesis and biological evaluation of pyrazole conjugated selenium Lumefantrine analogues
This study describes the synthesis and characterization of some 1-(2,7-dichloro-9-[(1,3-diphenyl-1H-pyrazol-4-yl)methylene]-9H-fluoren-4-yl)-2-(methylselenyl)-ethanols and their biological evaluation as antimicrobial agents. The synthesis of the target compounds requires two key starting materials, 1-[2,7-dichloro-9H-fluoren-4-yl]-2-(methylselanyl)ethan-1-ol and various 1,3-diarylpyrazole-4-carboxaldehydes. The key intermediates, 1,3-diarylpyrazole-4-carboxaldehydes were prepared by the Vilsmeier-Haack reaction. Finally, the target compounds were obtained by a simple Knoevenagel condensation. The structures of the newly synthesized compounds were established based on spectral techniques. The synthesized compounds were screened for their in vitro antibacterial, antifungal, and anti-inflammatory activities. All the compounds were tested for their preliminary cytotoxicity by hemolysis assay. The microbial growth inhibition was also investigated via in silico molecular docking studies. Graphical abstract.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2023 |
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| Erschienen: |
2023 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:20 |
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| Enthalten in: |
Journal of the Iranian Chemical Society - 20(2023), 8 vom: 28. Apr., Seite 1903-1916 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Puthran, Divyaraj [VerfasserIn] |
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| Links: |
Volltext [lizenzpflichtig] |
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| Themen: |
1,3-Diarylpyrazole-4-carboxaldehydes |
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| Anmerkungen: |
© Iranian Chemical Society 2023. Springer Nature or its licensor (e.g. a society or other partner) holds exclusive rights to this article under a publishing agreement with the author(s) or other rightsholder(s); author self-archiving of the accepted manuscript version of this article is solely governed by the terms of such publishing agreement and applicable law. |
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| doi: |
10.1007/s13738-023-02807-9 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
SPR052230198 |
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| 520 | |a This study describes the synthesis and characterization of some 1-(2,7-dichloro-9-[(1,3-diphenyl-1H-pyrazol-4-yl)methylene]-9H-fluoren-4-yl)-2-(methylselenyl)-ethanols and their biological evaluation as antimicrobial agents. The synthesis of the target compounds requires two key starting materials, 1-[2,7-dichloro-9H-fluoren-4-yl]-2-(methylselanyl)ethan-1-ol and various 1,3-diarylpyrazole-4-carboxaldehydes. The key intermediates, 1,3-diarylpyrazole-4-carboxaldehydes were prepared by the Vilsmeier-Haack reaction. Finally, the target compounds were obtained by a simple Knoevenagel condensation. The structures of the newly synthesized compounds were established based on spectral techniques. The synthesized compounds were screened for their in vitro antibacterial, antifungal, and anti-inflammatory activities. All the compounds were tested for their preliminary cytotoxicity by hemolysis assay. The microbial growth inhibition was also investigated via in silico molecular docking studies. Graphical abstract | ||
| 650 | 4 | |a 1,3-Diarylpyrazole-4-carboxaldehydes |7 (dpeaa)DE-He213 | |
| 650 | 4 | |a Vilsmeier–Haack reaction |7 (dpeaa)DE-He213 | |
| 650 | 4 | |a Anti-inflammatory |7 (dpeaa)DE-He213 | |
| 650 | 4 | |a Molecular docking |7 (dpeaa)DE-He213 | |
| 700 | 1 | |a Kamat, Vinuta |4 aut | |
| 700 | 1 | |a Purushotham, Nikil |4 aut | |
| 700 | 1 | |a Poojary, Boja |0 (orcid)0000-0001-6725-3289 |4 aut | |
| 700 | 1 | |a Rasheed, Mohammed Shafeeulla |4 aut | |
| 700 | 1 | |a Hegde, Hemant |4 aut | |
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