Synthesis and biological evaluation of hydantoin derivatives as potent antiplasmodial agents
Copyright © 2024 Elsevier Ltd. All rights reserved..
Malaria, a devastating disease, has claimed numerous lives and caused considerable suffering, with young children and pregnant women being the most severely affected group. However, the emergence of multidrug-resistant strains of Plasmodium and the adverse side effects associated with existing antimalarial drugs underscore the urgent need for the development of novel, well-tolerated, and more efficient drugs to combat this global health threat. To address these challenges, six new hydantoins derivatives were synthesized and evaluated for their in vitro antiplasmodial activity. Notably, compound 2c exhibited excellent inhibitory activity against the tested Pf3D7 strain, with an IC50 value of 3.97 ± 0.01 nM, three-fold better than chloroquine. Following closely, compound 3b demonstrated an IC50 value of 27.52 ± 3.37 µM against the Pf3D7 strain in vitro. Additionally, all the hydantoins derivatives tested showed inactive against human MCR-5 cells, with an IC50 value exceeding 100 μM. In summary, the hydantoin derivative 2c emerges as a promising candidate for further exploration as an antiplasmodial compound.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2024 |
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| Erschienen: |
2024 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:103 |
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| Enthalten in: |
Bioorganic & medicinal chemistry letters - 103(2024) vom: 01. Apr., Seite 129701 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Chin, Ee-Zhen [VerfasserIn] |
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| Links: |
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| Themen: |
3D7 strain |
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| Anmerkungen: |
Date Completed 01.04.2024 Date Revised 01.04.2024 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.bmcl.2024.129701 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM369744918 |
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| 520 | |a Copyright © 2024 Elsevier Ltd. All rights reserved. | ||
| 520 | |a Malaria, a devastating disease, has claimed numerous lives and caused considerable suffering, with young children and pregnant women being the most severely affected group. However, the emergence of multidrug-resistant strains of Plasmodium and the adverse side effects associated with existing antimalarial drugs underscore the urgent need for the development of novel, well-tolerated, and more efficient drugs to combat this global health threat. To address these challenges, six new hydantoins derivatives were synthesized and evaluated for their in vitro antiplasmodial activity. Notably, compound 2c exhibited excellent inhibitory activity against the tested Pf3D7 strain, with an IC50 value of 3.97 ± 0.01 nM, three-fold better than chloroquine. Following closely, compound 3b demonstrated an IC50 value of 27.52 ± 3.37 µM against the Pf3D7 strain in vitro. Additionally, all the hydantoins derivatives tested showed inactive against human MCR-5 cells, with an IC50 value exceeding 100 μM. In summary, the hydantoin derivative 2c emerges as a promising candidate for further exploration as an antiplasmodial compound | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a 3D7 strain | |
| 650 | 4 | |a Antiplasmodial activity | |
| 650 | 4 | |a Hydantoin derivatives | |
| 650 | 4 | |a MRC-5 cells | |
| 650 | 4 | |a Plasmodium falciparum | |
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| 700 | 1 | |a Chang, Wei-Jin |e verfasserin |4 aut | |
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| 700 | 1 | |a Liew, Sook Yee |e verfasserin |4 aut | |
| 700 | 1 | |a Lau, Yee-Ling |e verfasserin |4 aut | |
| 700 | 1 | |a Ng, Yee-Ling |e verfasserin |4 aut | |
| 700 | 1 | |a Nafiah, Mohd Azlan |e verfasserin |4 aut | |
| 700 | 1 | |a Kurz, Thomas |e verfasserin |4 aut | |
| 700 | 1 | |a Tan, Siow-Ping |e verfasserin |4 aut | |
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