Combinatorial Synthesis of Transition State Mimetic Inhibitor Using Asymmetric Aldol, Reaction
使用不对称羟醛反应组合合成过渡态模拟抑制剂
基本信息
- 批准号:13672211
- 负责人:
- 金额:$ 2.24万
- 依托单位:
- 依托单位国家:日本
- 项目类别:Grant-in-Aid for Scientific Research (C)
- 财政年份:2001
- 资助国家:日本
- 起止时间:2001 至 2002
- 项目状态:已结题
- 来源:
- 关键词:
项目摘要
An efficient method has been developed for the first solid phase synthesis of HTLV 1 protease inhibitors that contain hydroxyethylamine isostere as transitionslate mimetic. The synthetic procedure was designed to allow the evaluation of stereostmctureactivity relationships at the scissile site. All the possible configurations at the hydroxy and side chainbearing asymmetric centers of the isostere were constructed by an esterderived asymmetric aldol reaction. Each inhibitor containing the isostere backbone was synthesized on solid support using the newly developed succinate ester linker. The configuration at the hydroxy and side chainbearing asymmetric center showed remarkable effects on the inhibitory activity. The K_i value changed with approximately two orders of magnitude. This approach enables an efficient preparation of the inhibitors containing a transitionstate mimetic
首次固相合成了含有羟乙胺异构体的HTLV-1酶抑制剂。合成程序的设计是为了评估剪切点的立体结构反应性关系。异构体的羟基和侧链不对称中心的所有可能构型都是通过酯衍生的不对称Aldol反应构建的。使用新开发的琥珀酸酯连接剂在固体载体上合成了每一种含有异构体骨架的缓蚀剂。羟基和侧链不对称中心的构型对抑制活性有显著影响。K_i值的变化约为两个数量级。该方法能够有效地制备含有过渡态模拟物的缓蚀剂
项目成果
期刊论文数量(10)
专著数量(0)
科研奖励数量(0)
会议论文数量(0)
专利数量(0)
K,Akaji, K,Teraya, S,Aimoto: "Stereoselective synthesis and evaluation of HTLV-1 protease inhibitors"Peptide Scaerice 2002. 37-40 (2003)
K,Akaji,K,Teraya,S,Aimoto:“HTLV-1蛋白酶抑制剂的立体选择性合成和评价”Peptide Scaerice 2002. 37-40 (2003)
- DOI:
- 发表时间:
- 期刊:
- 影响因子:0
- 作者:
- 通讯作者:
K.Teruya, T.Kawakami, K.Akaji, S.Aimoto: "Synthesis of [L40I, C90A, C109A]-human T-cell leukemia virus-type 1 protease"Tetrahedron Letters. (in press).
K.Teruya、T.Kawakami、K.Akaji、S.Aimoto:“[L40I、C90A、C109A]-人 T 细胞白血病病毒 1 型蛋白酶的合成”四面体字母。
- DOI:
- 发表时间:
- 期刊:
- 影响因子:0
- 作者:
- 通讯作者:
K.Teruya, T.Kawakami, K.Akaji, S.Aimoto: "Total synthesis of [L40I, C9OA, C109A]-human T-cell leukemia virus type 1 protease"Tetrahedron Letters. 43. 1487-1490 (2002)
K.Teruya、T.Kawakami、K.Akaji、S.Aimoto:“[L40I、C9OA、C109A]-人 T 细胞白血病病毒 1 型蛋白酶的全合成”四面体字母。
- DOI:
- 发表时间:
- 期刊:
- 影响因子:0
- 作者:
- 通讯作者:
K.Akaji, K.Teruya, S.Aimoto: "Stereoselective synthesis and evaluation of HTLV-1 protease inhibitors"Peptide Science 2002. 2002. 37-40 (2003)
K.Akaji、K.Teruya、S.Aimoto:“HTLV-1蛋白酶抑制剂的立体选择性合成和评价”肽科学2002. 2002. 37-40 (2003)
- DOI:
- 发表时间:
- 期刊:
- 影响因子:0
- 作者:
- 通讯作者:
K.Akaji, K.Teruya, S.Aimoto: "Solid-phase synthesis of HTLV-1 protease inhibitors containing hydroxyethylamine dipeptide isostere"Journal of the Organic Chemistry. 2003(In press). (2003)
K.Akaji、K.Teruya、S.Aimoto:“含羟乙胺二肽电子等排体的 HTLV-1 蛋白酶抑制剂的固相合成”有机化学杂志。
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- 影响因子:0
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AKAJI Kenichi其他文献
AKAJI Kenichi的其他文献
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{{ truncateString('AKAJI Kenichi', 18)}}的其他基金
Development of a novel persistent protease inhibitor containing D-amino acid
含D-氨基酸的新型持久性蛋白酶抑制剂的开发
- 批准号:
21590017 - 财政年份:2009
- 资助金额:
$ 2.24万 - 项目类别:
Grant-in-Aid for Scientific Research (C)
Development of SARS virus inhibitor using unusual amino acid-containing natural products as seeds
以含有罕见氨基酸的天然产物为种子开发SARS病毒抑制剂
- 批准号:
18590010 - 财政年份:2006
- 资助金额:
$ 2.24万 - 项目类别:
Grant-in-Aid for Scientific Research (C)
Intramolecularcyclization by solid-phase olefination and its application to combinatorial synthesis
固相烯化分子内环化及其在组合合成中的应用
- 批准号:
10557210 - 财政年份:1998
- 资助金额:
$ 2.24万 - 项目类别:
Grant-in-Aid for Scientific Research (B)
Convergent synthesis and SAR of dolastatin 15 by solid phase coupling
固相偶联聚合合成多拉司他汀15及比吸收率
- 批准号:
10672011 - 财政年份:1998
- 资助金额:
$ 2.24万 - 项目类别:
Grant-in-Aid for Scientific Research (C)
Convergent Synthesis of Anti-Cancer Alkaloid, Mirabazols, using a New Coupling Reagent
使用新型偶联剂聚合合成抗癌生物碱米拉巴唑
- 批准号:
08672459 - 财政年份:1996
- 资助金额:
$ 2.24万 - 项目类别:
Grant-in-Aid for Scientific Research (C)
Development of Low Molecular Weight HIV Protease Inhibitor for Oral Use
口服低分子量HIV蛋白酶抑制剂的研制
- 批准号:
07557141 - 财政年份:1995
- 资助金额:
$ 2.24万 - 项目类别:
Grant-in-Aid for Scientific Research (B)
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