title: Natural products in combinatorial chemistry: an andrographolide-based library.
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.
authors.affiliation: Analyticon Discovery GmbH, Hermannswerder Haus 17, 14473 Potsdam, Germany. c.mang@ac-discovery.com
authors.forename: Christian
authors.initials: C
authors.lastname: Mang
authors.forename: Sven
authors.initials: S
authors.lastname: Jakupovic
authors.forename: Stefan
authors.initials: S
authors.lastname: Schunk
authors.forename: Horst-Dieter
authors.initials: HD
authors.lastname: Ambrosi
authors.forename: Oliver
authors.initials: O
authors.lastname: Schwarz
authors.forename: Jasmin
authors.initials: J
authors.lastname: Jakupovic
mesh_terms: D001688:Biological Products / Q000138:chemical synthesis*; D020650:Combinatorial Chemistry Techniques / Q000379:methods*; D004224:Diterpenes / Q000737:chemistry*; D007202:Indicators and Reagents; D008958:Models, Molecular
chemical_list: D001688:Biological Products; D004224:Diterpenes; D007202:Indicators and Reagents; C030419:andrographolide