Chapter 10: The Challenges of Multi-Target Lead Optimization
Published:28 Mar 2012
Special Collection: 2012 ebook collection , 2011-2015 industrial and pharmaceutical chemistry subject collectionSeries: Drug Discovery
During multi-target lead optimization, medicinal chemists must address three principal challenges. First, the various desired activities must be adequately balanced and the activity profile of any active metabolites must also be considered. Second, undesired activities associated with side effects need to be removed. Third, a pharmacokinetic profile appropriate for the desired route of administration, usually oral, must be obtained. Given the extent of these challenges, the need for a high quality lead compound is paramount.