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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 pseudo-peptides with drug properties. As such, it includes peptoids, beta-peptides, polyamide DNA binders as well as peptide nucleic acids. The expert authors and editor 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.