書誌事項
- タイトル別名
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- Development for Peptidomimetic Chemistry based on Chloroalkene Structures
説明
<p>In drug discovery, various biologically active peptides have been discovered, characterized and modified for medicinal chemistry. However, the utilization of peptides as therapeutics has some limitation owing to several factors, including low metabolic stability towards proteolysis and undesired interactions with multiple receptors. Hence, the development of “peptidomimetc”, in which a part or whole of a molecule is modified, is an important strategy with which to enhance the stability or bioactivity of peptide-based drugs. In this situation, we have designed and developed a synthetic method for chloroalkene dipeptide isosteres (CADIs), which involves replacement of an amide bond in peptides with a chloroalkene structure, toward the peptidomimetc. By a developed synthetic method, an N-tert-butylsulfonyl protected CADI was obtained utilizing diastereoselective allylic alkylation with organocopper reagents as a key reaction. This CADI was also transformed into an N-Fmoc protected CADI in a few steps. In addition, The CADI could be used in Fmoc-based solid-phase peptide synthesis and applied to introduce for a bioactive peptide.</p>
収録刊行物
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- 有機合成化学協会誌
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有機合成化学協会誌 77 (9), 904-911, 2019-09-01
公益社団法人 有機合成化学協会
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詳細情報 詳細情報について
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- CRID
- 1390001277348436736
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- NII論文ID
- 130007705928
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- ISSN
- 18836526
- 00379980
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- 本文言語コード
- ja
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- 資料種別
- journal article
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- データソース種別
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- JaLC
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- CiNii Articles
- KAKEN
- OpenAIRE
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- 抄録ライセンスフラグ
- 使用不可
