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Drug Discovery
Designing Multi-Target Drugs
Hardback ISBN:
978-1-84973-362-5
PDF ISBN:
978-1-84973-491-2
Special Collection:
2012 ebook collection
,
2011-2015 industrial and pharmaceutical chemistry subject collection
Series:
Drug Discovery
No. of Pages:
394
Publication date:
28 Mar 2012
Book Chapter
Chapter 10: The Challenges of Multi-Target Lead Optimization
By
J. Richard Morphy
J. Richard Morphy
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Published:28 Mar 2012
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Special Collection: 2012 ebook collection , 2011-2015 industrial and pharmaceutical chemistry subject collectionSeries: Drug Discovery
Page range:
141 - 154
Citation
J. Richard Morphy, in Designing Multi-Target Drugs, ed. J. R. Morphy and C. J. Harris, The Royal Society of Chemistry, 2012, ch. 10, pp. 141-154.
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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.
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