Design and synthesis of peptide-based macrocyclic cyclophilin inhibitors

被引：4

作者：

Granger, Brett A. ^{[1
]}

Brown, Dean G. ^{[1
]}

机构：

[1] AstraZeneca R&D Boston, Infect Innovat Med Unit, Waltham, MA 02451 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2016年 / 26卷 / 21期

关键词：

Peptidyl-prolyl isomerases; Cyclophilin; Macrocycle; Ring-closing metathesis; ALKYLATION; ACID;

D O I：

10.1016/j.bmcl.2016.09.039

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The efficient assembly of an 18-membered macrocyclic peptide core was realized by a straightforward and convergent approach utilizing ring-closing metathesis of the corresponding linear tetrapeptides as the key transformation. This approach allowed for the facile preparation of a focused library of novel macrocycles that culminated in the discovery of a cyclophilin A inhibitor with a K-d = 5.4 mu M. (C) 2016 Elsevier Ltd. All rights reserved.

引用

页码：5304 / 5307

页数：4

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