Synthesis and in vitro antiprotozoal evaluation of novel metronidazole–Schiff base hybrids Article Swipe
Richard M. Beteck
,
Michelle Isaacs
,
Lesetja J. Legoabe
,
Heinrich C. Hoppe
,
Christina C. Tam
,
Jong H. Kim
,
Jacobus P. Petzer
,
Luisa W. Cheng
,
Quincel Quiambao
,
Kirkwood M. Land
,
Setshaba D. Khanye
·
YOU?
·
· 2022
· Open Access
·
· DOI: https://doi.org/10.1002/ardp.202200409
YOU?
·
· 2022
· Open Access
·
· DOI: https://doi.org/10.1002/ardp.202200409
Herein we report the synthesis of 21 novel small molecules inspired by metronidazole and Schiff base compounds. The compounds were evaluated against Trichomonas vaginalis and cross‐screened against other pathogenic protozoans of clinical relevance. Most of these compounds were potent against T. vaginalis , exhibiting IC 50 values < 5 µM. Compound 20 , the most active compound against T. vaginalis , exhibited an IC 50 value of 3.4 µM. A few compounds also exhibited activity against Plasmodium falciparum and Trypanosomal brucei brucei , with compound 6 exhibiting an IC 50 value of 0.7 µM against P. falciparum and compound 22 exhibiting an IC 50 value of 1.4 µM against T.b. brucei . Compound 22 is a broad‐spectrum antiprotozoal agent, showing activities against all three pathogenic protozoans under investigation.
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Metadata
- Type
- article
- Language
- en
- Landing Page
- https://doi.org/10.1002/ardp.202200409
- https://onlinelibrary.wiley.com/doi/pdfdirect/10.1002/ardp.202200409
- OA Status
- hybrid
- Cited By
- 5
- References
- 40
- Related Works
- 10
- OpenAlex ID
- https://openalex.org/W4310456610
All OpenAlex metadata
Raw OpenAlex JSON
- OpenAlex ID
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https://openalex.org/W4310456610Canonical identifier for this work in OpenAlex
- DOI
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https://doi.org/10.1002/ardp.202200409Digital Object Identifier
- Title
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Synthesis and in vitro antiprotozoal evaluation of novel metronidazole–Schiff base hybridsWork title
- Type
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articleOpenAlex work type
- Language
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enPrimary language
- Publication year
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2022Year of publication
- Publication date
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2022-11-29Full publication date if available
- Authors
-
Richard M. Beteck, Michelle Isaacs, Lesetja J. Legoabe, Heinrich C. Hoppe, Christina C. Tam, Jong H. Kim, Jacobus P. Petzer, Luisa W. Cheng, Quincel Quiambao, Kirkwood M. Land, Setshaba D. KhanyeList of authors in order
- Landing page
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https://doi.org/10.1002/ardp.202200409Publisher landing page
- PDF URL
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https://onlinelibrary.wiley.com/doi/pdfdirect/10.1002/ardp.202200409Direct link to full text PDF
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YesWhether a free full text is available
- OA status
-
hybridOpen access status per OpenAlex
- OA URL
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https://onlinelibrary.wiley.com/doi/pdfdirect/10.1002/ardp.202200409Direct OA link when available
- Concepts
-
Antiprotozoal, Trichomonas vaginalis, Trypanosoma brucei, Plasmodium falciparum, Metronidazole, Chemistry, In vitro, Trichomoniasis, Stereochemistry, Microbiology, Pharmacology, Antibiotics, Biochemistry, Biology, Medicine, Malaria, Immunology, Pathology, GeneTop concepts (fields/topics) attached by OpenAlex
- Cited by
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5Total citation count in OpenAlex
- Citations by year (recent)
-
2025: 1, 2024: 4Per-year citation counts (last 5 years)
- References (count)
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40Number of works referenced by this work
- Related works (count)
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10Other works algorithmically related by OpenAlex
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