Synthesis of Squaric Acid Monoamides as Building Blocks for Drug Discovery

被引：1

作者：

Long, Nathan ^{[1
]}

Le Gresley, Adam ^{[1
]}

Solomonsz, Arran ^{[2
]}

Wozniak, Antony ^{[2
]}

Brough, Steve ^{[3
]}

Wren, Stephen P. ^{[1
]}

机构：

[1] Kingston Univ, Fac Hlth Sci Social Care & Educ, Sch Life Sci Pharm & Chem, Penrhyn Rd, Kingston Upon Thames KT1 2EE, England

[2] Asynt Ltd, Hall Barn Rd Ind Estate,Hall Barn Rd, Ely CB7 5RJ, England

[3] Key Organ Ltd, Highfield Rd Insutrial Estate Camelford, Cornwall PL32 9RA, England

来源：

SYNOPEN | 2023年 / 07卷 / 03期

关键词：

squaric acid; squaramide; bioisostere; carboxylic acid; compound library; BIOISOSTERIC MODIFICATIONS; SQUARAMIDES; DERIVATIVES; MOLECULES; ANALOGS;

D O I：

10.1055/a-2148-9518

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Herein, we present a synthetic compound library compris-ing of 28 anilino and benzylamino monosquarate-amide derivatives. Members of this library were designed as bioisosteric replacements for groups such as the ubiquitous carboxylic acid moiety. Further to their synthesis, we have shown the potential of these chemical building blocks for the generation of additional novel compounds. This work forms part of our efforts aimed at the assembly of 96-well plates loaded with bioisosteric analogues that may be used to enrich drug discovery programs. The research presented in this work focuses on the chemistry of 3,4-dihydroxycyclobut-3-ene-1,2-dione, a known carboxylic acid bioisostere.

引用

页码：401 / 407

页数：7

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