Library strategies

R. Wischnat, R. Martin, S. Takayama, C.-H. Wong, Che-moenzymatic Synthesis of Iminocyclitol Derivatives A Useful Library Strategy for the Development of Selective Fucosyltransfer Enzymes Inhibitors , Bioorg. Med, Chan. Lett. 1998, 8, 3353-3358. 

One approach to screening subsets of available compounds is to screen sets of compounds that, although not representative of the molecular diversity of the available compound collection, do contain as much structure activity relationship information as possible. An example of this was the Informer Library strategy proposed by CombiChem (which was eventually purchased by DuPont Pharmaceuticals in 1999) (23). Unfortunately, there have been no published applications of this screening strategy that assess its success or failure. 

Figure 6.11 Typical tridentate ligand structure incorporating a chiral amino alcohol and modified diamine-based tridentate ligand structure attached to the solid support for parallel catalyst library strategy.

However, the properties of the new complexes derived from these projects have not been investigated. Furthermore it is questionable whether this approach allows the discovery of new catalysts because the screening procedure led to the most stable complexes. However stability is a property that does not favor catalytic activity. Nevertheless, a recent study by the same authors revealed that libraries made by this approach can indeed point at least towards new lead structures for catalysts [7]. For the identification of efficient catalysts from a large library, strategies of parallel... 

Omission library Strategy for identifying active library members by the systematic omission of building blocks from mixtures. Observation of reduced activity in a certain pool suggests that the building block that was omitted in that pool contributes to activity. 

In conclusion, there have been several successful approaches to implementing a purified library strategy to maximize the value of natural product sources. Each of these approaches has been enhanced by the integration of mass spectrometry. The further evolution of this strategy is still in progress. 

Designed antimicrobials from host defense peptides using multivalent and combinatorial library strategies... 

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