Synthesis and in vivo antimalarial evaluation of novel hydroxyethylamine derivatives
A series of hydroxyethylamines has been synthesized from the reaction of (2S,3S )Boc-phenylalanine epoxide with alkyl amines in good yields and evaluated for their in vivo antimalarial activity in mice. Compound 4g presented better activity then the reference artesunate in percentage of inhibition of parasitemia in treated P. berghei-infected mice and compare to the activity of artesunate in the survival of mice 14 days after infection. In addiction, no hemolytic activity was found, which supports that inhibition of parasitemia is due to antimalarial activity. The compound 4g inhibited the differentiation to schizonts suggesting that parasite metabolism is a possible target of 4g. These results indicate that this class of compound possesses promising perspectives for the development of new antimalarial drugs.
| Medienart: |
E-Artikel |
|---|
| Erscheinungsjahr: |
2012 |
|---|---|
| Erschienen: |
2012 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:8 |
|---|---|
| Enthalten in: |
Medicinal chemistry (Shariqah (United Arab Emirates)) - 8(2012), 2 vom: 28. März, Seite 266-72 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
de Souza, Mariana Conceição [VerfasserIn] |
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| Themen: |
Antimalarials |
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| Anmerkungen: |
Date Completed 05.11.2012 Date Revised 10.12.2019 published: Print Citation Status MEDLINE |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM215896424 |
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| 245 | 1 | 0 | |a Synthesis and in vivo antimalarial evaluation of novel hydroxyethylamine derivatives |
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| 500 | |a published: Print | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a A series of hydroxyethylamines has been synthesized from the reaction of (2S,3S )Boc-phenylalanine epoxide with alkyl amines in good yields and evaluated for their in vivo antimalarial activity in mice. Compound 4g presented better activity then the reference artesunate in percentage of inhibition of parasitemia in treated P. berghei-infected mice and compare to the activity of artesunate in the survival of mice 14 days after infection. In addiction, no hemolytic activity was found, which supports that inhibition of parasitemia is due to antimalarial activity. The compound 4g inhibited the differentiation to schizonts suggesting that parasite metabolism is a possible target of 4g. These results indicate that this class of compound possesses promising perspectives for the development of new antimalarial drugs | ||
| 650 | 4 | |a Evaluation Study | |
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
| 650 | 7 | |a Antimalarials |2 NLM | |
| 650 | 7 | |a Ethylamines |2 NLM | |
| 700 | 1 | |a Gonçalves-Silva, Triciana |e verfasserin |4 aut | |
| 700 | 1 | |a Moreth, Marcele |e verfasserin |4 aut | |
| 700 | 1 | |a Gomes, Claudia R B |e verfasserin |4 aut | |
| 700 | 1 | |a Kaiser, Carlos Roland |e verfasserin |4 aut | |
| 700 | 1 | |a de Oliveira Henriques, Maria das Graças Muller |e verfasserin |4 aut | |
| 700 | 1 | |a de Souza, Marcus V N |e verfasserin |4 aut | |
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