N-to-C Solid-Phase Peptide and Peptide Trifluoromethylketone Synthesis Using Amino Acid tert-Butyl Esters.
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- Gutheil William G.
- Division of Pharmaceutical Sciences, School of Pharmacy, University of Missouri-Kansas City
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- Xu Qingchai
- Division of Pharmaceutical Sciences, School of Pharmacy, University of Missouri-Kansas City
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抄録
Solid-phase peptide synthesis in the N-to-C direction, opposite to the classical C-to-N direction of peptide synthesis, provides the synthetically versatile C-terminal carboxyl group for further modification into C-terminally modified peptide mimetics. These are of general interest as potential bioactive agents, particularly as protease inhibitors. Elaboration of peptide mimetics on the solid-phase would facilitate synthesis of peptide mimetic combinatorial libraries. This report describes an effective strategy for solid-phase inverse peptide synthesis based on readily available amino acid tert-butyl esters. The potential of this approach for peptide mimetic synthesis is demonstrated by the solid-phase synthesis of two peptide trifluoromethylketones.
収録刊行物
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- CHEMICAL & PHARMACEUTICAL BULLETIN
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CHEMICAL & PHARMACEUTICAL BULLETIN 50 (5), 688-691, 2002
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
- 1390001204164137728
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- NII論文ID
- 110003616229
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- NII書誌ID
- AA00602100
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- COI
- 1:CAS:528:DC%2BD38Xks12ksrk%3D
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- ISSN
- 13475223
- 00092363
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- NDL書誌ID
- 6155850
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- PubMed
- 12036033
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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
- Crossref
- PubMed
- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可