ABSTRACT
Combinatorial chemistry is designed to support the lead discovery process. It is a technique by which a large number of structurally distinct molecules can be synthesized together at a time and submitted for focused or varied pharmacological assay. Combinatorial chemistry has enabled the identification of many leads in drug discovery programs. An ideal combinatorial library should be relatively small and should contain chemically and functionally diverse compounds; each having a distinct biological activity, oral bioavailability and less toxicity. Combinatorial chemistry can contribute to drug discovery by helping to identify biologically active compounds in conjunction with high-throughput screening thus accelerating the discovery of lead compounds with a desired pharmacological profile. Combinatorial chemistry has the power to generate highly diverse compound collections for random screening. The impact of combinatorial chemistry on lead identification is dictated by the size and composition of the library.
