Natural Chromenes and Chromene Derivatives as Potential Anti-trypanosomal Agents
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- Batista Jr. João Marcos
- Instituto de Química, Universidade Estadual Paulista (UNESP)
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- Lopes Adriana Aparecida
- Instituto de Química, Universidade Estadual Paulista (UNESP)
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- Ambrósio Daniela Luz
- Faculdade de Ciências Farmacêuticas, Universidade Estadual Paulista (UNESP)
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- Regasini Luis Octávio
- Instituto de Química, Universidade Estadual Paulista (UNESP)
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- Kato Massuo Jorge
- Instituto de Química, Universidade de São Paulo
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- Bolzani Vanderlan da Silva
- Instituto de Química, Universidade Estadual Paulista (UNESP)
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- Cicarelli Regina Maria Barretto
- Faculdade de Ciências Farmacêuticas, Universidade Estadual Paulista (UNESP)
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- Furlan Maysa
- Instituto de Química, Universidade Estadual Paulista (UNESP)
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説明
The aim of the study was to investigate the anti-trypanocidal activities of natural chromene and chromene derivatives. Five chromenes were isolated from Piper gaudichaudianum and P. aduncum, and a further seven derivatives were prepared using standard reduction, methylation and acetylation procedures. These compounds were assayed in vitro against epimastigote forms of Trypanosoma cruzi, the causative agent of Chagas disease. The results showed that the most of the compounds, especially those possessing electron-donating groups as substituents on the aromatic ring, showed potent trypanocidal activity. The most active compound, [(2S)-methyl-2-methyl-8-(3″-methylbut-2″-enyl)-2-(4′-methylpent-3′-enyl)-2H-chromene-6-carboxylate], was almost four times more potent than benznidazole (the positive control) and showed an IC50 of 2.82 μM. The results reveal that chromenes exhibit significant anti-trypanocidal activities and indicate that this class of natural product should be considered further in the development of new and more potent drugs for use in the treatment of Chagas disease.
収録刊行物
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- Biological & Pharmaceutical Bulletin
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Biological & Pharmaceutical Bulletin 31 (3), 538-540, 2008
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390001204625968512
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- NII論文ID
- 110006623091
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- NII書誌ID
- AA10885497
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- ISSN
- 13475215
- 09186158
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- NDL書誌ID
- 9393515
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDLサーチ
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