Generating compound library

The Ugi four-component condensation (U-4CC) between an aldehyde, an amine, a carboxylic acid and an isocyanide allows the rapid preparation of a-aminoacyl amide derivatives. The Ugi Reaction products can exemplify a wide variety of substitution patterns, and constitute peptidomimetics that have potential pharmaceutical applications. This reaction is thus very important for generating compound libraries for screening purposes. 

Furthermore, a number of approaches were developed to generate compound libraries that incorporate natural product information. For example, natural molecules (specifically, selected... 

Combinatorial chemistry (Section 27.18) A method for carrying out a large number of reactions on a small scale in the solid phase so as to generate a library of related compounds for further study, such as biological testing. 

Cathepsin D. The design of inhibitors of the aspartyl protease cathepsin D started from a virtual library of peptide analogs that contained the typical hydroxyethylamine isoster for the cleavable peptide bond. As the availability of starting materials would have generated a library of about 1 billion compounds, virtual screening was applied to reduce this multitude of candidate structures to a reasonable number. The backbone of a peptide... 

In closely related work, similar solid-phase chemistry was employed by the same research group to prepare biaryl urea compound libraries by microwave-assisted Suzuki couplings followed by cleavage from the resin with amines (Scheme 7.47) [18]. The above described procedure enabled the generation of large biaryl urea compound libraries employing a simple domestic microwave oven. 

---