The Challenges of Multi-Target Lead Optimization
John Richard Morphy · Royal Society of Chemistry eBooks · 2012
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.