Natural products in combinatorial chemistry: an andrographolide-based library |
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Authors: | Mang Christian Jakupovic Sven Schunk Stefan Ambrosi Horst-Dieter Schwarz Oliver Jakupovic Jasmin |
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Affiliation: | Analyticon Discovery GmbH, Hermannswerder Haus 17, 14473 Potsdam, Germany. c.mang@ac-discovery.com |
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Abstract: | 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. |
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