Creative and Unexpected Solutions

Besides the use of novel fiinctionahty that is beyond rational design by synthetic chemists, nature is unsurpassed at the display of chemical information in three-dimensional space. For example, despite intensive efforts, there is no standard algorithm for translating a linear peptide into a small-molecule peptidomimetic. Meanwhile, numerous natural scaffolds perform this task efficiently, as in the opium alkaloids conformational mimicry of the enkephaUns. We will never know what revolutionary new scaffolds and pharmacophores will be lost if natural product screening is discontinued. 

Combinatorial Synthesis of Natural Product-Based Libraries 

Average Values (Rounded to Whole Integer unless Inappropriate) for Properties in Drugs, Natural, and Seminatural Compounds, Natural Products, and Combinatorial Compounds 

Property Drugs Natural or Seminatural Natural Combin, 

Source Adapted from Feher, M. and Schmidt, J.M., Property distributions differences between drugs, natural products, and molecules from combinatorial chemistry, J. Cherru Inf. CompuL 

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