An improved synthesis of haloacetamidine-based inactivators of protein arginine deiminase 4 (PAD4)

被引：23

作者：

Causey, Corey P. ^{[1
]}

Thompson, Paul R. ^{[1
]}

机构：

[1] Univ S Carolina, Dept Chem & Biochem, Columbia, SC 29208 USA

来源：

TETRAHEDRON LETTERS | 2008年 / 49卷 / 28期

关键词：

D O I：

10.1016/j.tetlet.2008.05.021

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Protein arginine deiminase 4 (PAD4) is an enzyme that hydrolyzes peptidyl arginine residues to form citrulline and ammonia. This enzyme has been implicated in several disease states, for example, rheumatoid arthritis, and therefore represents a unique target for the development of a novel therapeutic. A solution-phase synthesis of Cl-amidine, the most potent PAD4 inactivator described to date, has been developed. This synthesis proceeds in 80% yield over four steps at a significantly (12-fold) lower cost. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：4383 / 4385

页数：3

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