Natural products in combinatorial chemistry: An andrographolide-based library

被引：34

作者：

Mang, C ^{[1
]}

Jakupovic, S ^{[1
]}

Schunk, S ^{[1
]}

Ambrosi, HD ^{[1
]}

Schwarz, O ^{[1
]}

Jakupovic, J ^{[1
]}

机构：

[1] Analyt Discovery GmbH, D-14473 Potsdam, Germany

来源：

JOURNAL OF COMBINATORIAL CHEMISTRY | 2006年 / 8卷 / 02期

关键词：

D O I：

10.1021/cc050143n

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

The generation of a natural-product-based library starting from andrographolide is described. Utilizing andrographolide itself in parallel solution-phase synthesis leads to a 360-membered library. The initial transformation of the starting material via ozonolysis is followed by the conversion into a suitable template by introduction of a thiazole moiety. Subsequent decoration at two points of diversity yields the desired natural product derivatives. The selection of actually synthesized compounds is based on a virtually generated library and the assessment of its members with respect to physicochemical parameters, thus ensuring pharmacological relevance of the compounds.

引用

页码：268 / 274

页数：7

共 27 条

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