Organic Synthesis (Combinatorial Chemistry) for Drug Discovery

As mentioned above, modern drug discovery often involves synthesis of a large number of small molecules that constitute a combinatorial library. These molecules may be synthesized keeping a target molecule in mind or else may be synthesized as complex and diverse set of molecules without regard to any particular target molecule. These two approaches used for organic synthesis of molecules for drug discovery are described as target-oriented and diversity-oriented organic syntheses and will be discussed separately. In target-oriented approach, the protein target is known, but the compound with high affinity to this target need to be identified, so that the synthesis of this putative drug compound can be planned using an approach described as retrosynthesis analysis. In diversity-oriented approach, on the other hand, the protein target and the small molecules (putative drug) that would regulate a specified biosynthetic pathway are identified simultaneously using a combinatorial library.