Parallel synthesis is fond of connecting chemistries that can rapidly create a scaffold able to dispose the diversity elements in 3D positions. Dihydroquinazolinones belong to this family. Starting from isatoic anhydride or analogs, the heterocycle is produced in two steps using amines and aldehydes, two of the most diverse families of building blocks. Since the diversity elements are in a short connectivity distance in a rigid cycle, the final molecules adopt a 3D structure able to interact with complex active sites.

It is not surprising to see many applications for this scaffold. In the Pubchem database, for the 414 dihydroquinazolinones having been tested in at least one assay, 329 hits are described in screenings against receptors as diverse as proteases, kinases, GPCRs or protein-protein interaction. Molecules on the market sharing the structure belong to the thiazide diuretic family. Other applications are described in the literature and are discussed in the brochure of the library.

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