Purine scaffold-based library

Another approach followed by Wang et al. led to an inhibitor of Tritrichomonas foetus hypoxanthine-guanine-xanthine phosphoribosyltransferase (HGXPRT). The X-ray structure of this enzyme is available and it was used in a search for novel scaffolds. The Available Chemicals Directory (ACD) was screened with the program DOCK. Isatin and phthalic anhydride were capable of mimicking the substrate purine base and acting as competitive inhibitors. A virtual library of substituted... 

Chemical genetics is an emerging field that offers powerful tools to search for novel drug candidates and their targets. The design of a tagged library was based on a triazine scaffold 352 due to its ease of manipulation and structural similarity to purine and pyrimidine, which have already been demonstrated to be active in various biological systems (Scheme 80). In addition, the triazine scaffold has threefold symmetry, and the positional modification is much more flexible than that in the purines or pyrimidines. 

Monocyclic and Bicyclic aromatic heterocycles such as imidazoles, thiazoles, thiadiazoles, oxazoles, oxadiazoles quinazolines, indoles, benzimidazoles, purines pyrido[43-d]pyri-midines, thiazolo[5,4-d]pyrimidines, thiazolo[4,5-d]pyrimidines, oxazolo[5,4-d]pyrimi-dines and thieno[2,3-d]pyrimidines are renowned pharmacophores in drug discovery. These special structures are well explained and exemplified in chemical compound libraries. In this chapter, several types of thiazole based heterocyclic scaffolds such as mono-cyclic or bicyclic systems synthesis and their biological activities studies are presented, which are not frequently present in books and reviews. We mention the first importance of synthetic route of various thiazole based compounds and their applications in medicinal chemistry in this chapter. 

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