Drug discovery is devoted to the topic and draws together knowledge gained on different types of peptidomimetics and other pseudo-peptides with drug properties. It includes peptoides (N-substituted oligoglycines) beta-peptides, gamma-peptides, pyrrole-imidazole polyamides, DNA-like peptide nucleic acids, Alpha-helical peptide nucleic acids, DNA-cleaving pseudo-peptides in DNA binders as well as peptide nucleic acids. Peptides are among the most versatile bioactive molecules, yet they do not make good drugs, because they are quickly degraded or modified in the body. Thus, drug discovery has turned to the novel field of peptidomimetics to design non-peptide compounds mimicking the pharmacophore and thus the activity of the original peptide. These novel compounds open up new perspectives in drug design by providing an entire range of highly specific pharmaceuticals that have a high bioavailability. Peptides are among the most versatile bioactive molecules, yet the do not make good drugs, because they are quickly degraded or modified in the body. To overcome this problem, stable and at the same time biologically active pseudo-peptides have been developed. These novel compounds open up new perspectives in drug design by providing an entire range of highly specific and non-toxic pharmaceuticals. This is the first work devoted to the topic and draws together knowledge gained on different types of Peptidomimetics and other pseudopeptides with drug properties. As such, it includes peptoids, beta-peptides, polyamide DNA binders as well as peptide nucleic acids. The experts in the field of cheminformatics, chemogenomics, proteomics and genomics discuss chemical properties and stability, biological activity and reactivity, as well as practical aspects of synthesis, making this a prime resource for drug developers and bioorganic chemists working with these compounds.