Total synthesis of a Pepstatin analogue incorporating two trifluoromethyl hydroxymethylene isosteres

被引：12

作者：

Pesenti, C

Arnone, A

Aubertin, AM

Bravo, P

Frigerio, M

Panzeri, W

Schmidt, S

Viani, F

Zanda, M

机构：

[1] CNR, Ctr Studio Sostanze Organ Nat, I-20131 Milan, Italy

[2] Politecn Milan, Dipartimento Chim, I-20131 Milan, Italy

[3] INSERM, U74, Inst Virol, F-67000 Strasbourg, France

来源：

TETRAHEDRON LETTERS | 2000年 / 41卷 / 37期

关键词：

peptide mimetics; enzyme inhibitors; Pepstatin; trifluoromethyl group;

D O I：

10.1016/S0040-4039(00)01244-2

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The total synthesis of a trifluoromethyl (Tfm) analogue of the aspartate protease inhibitor Pepstatin has been accomplished via incorporation of two alpha-Tfm-amino beta-hydroxy peptide isosteres instead of the natural statine units. The title compound as well as several Tfm-substituted precursors did not show anti-HIV activity. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

收藏

页码：7239 / 7243

页数：5

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