Abstract
After the optimization of a lead structure there are still problems. Many substances lack important characteristics that are required for therapy in humans, for instance adequate bioavailability, duration of action and metabolic stability, the ability to penetrate the blood–brain barrier, selectivity, or good tolerability. Often it proves impossible to address or improve these properties through structural variation. Then a detour can be taken over special preparations, for instance with poorly water-soluble substances, or over a derivatization to a prodrug. This term refers to a non-active or poorly active precursor or derivative of an active molecule. In the organism this form is converted to the actual active substance. In most cases, this is achieved by enzymatic reactions, in a few cases it happens by spontaneous chemical decomposition.
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Klebe, G. (2013). Designing Prodrugs. In: Klebe, G. (eds) Drug Design. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-17907-5_9
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DOI: https://doi.org/10.1007/978-3-642-17907-5_9
Publisher Name: Springer, Berlin, Heidelberg
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