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• W1530801019 abstract "Choosing from different methods of screening and identifying active compounds from combinatorial mixtures depends on a comparison of the costs and benefits of resynthesizing, retesting, coding, and using direct analytical chemistry. The search for new compounds with therapeutic activity commonly begins with the serendipitous discovery of an active lead compound in a large random compound library. In such purpose, when a relatively new collection of techniques and ideas are used, all generally aimed at producing very large sets of compounds for use in drug discovery, it is termed as “combinatorial chemistry.” Research is continuing on a variety of methods in combinatorial chemistry and the screening of compounds synthesized by combinatorial chemistry. This chapter discusses the more specific issues relating to screening mixtures of compounds that are produced by combinatorial synthesis. An ideal compound screening method, in theory, would quickly provide robust information on the activity of every compound tested while being able to handle very large numbers of compounds. Parallel screening of individual compounds in high density arrays is commonly used with this ideal in mind. Combinatorial chemistry has enabled chemists to synthesize a greater number of compounds than have been traditionally screened with these methods and these compounds are produced in mixtures. This has resulted in a compromise, in which the vast numbers of compounds that can be synthesized as combinatorial mixture, are subjected to screening techniques that require deconvolution, decoding, or other specialized methods to identify those compounds that have a desired biological activity. The quality of the method of deconvolution or identification, in general, determines whether this compromise is successful in increasing the rate of discovery of useful compounds. Screening small mixtures of compounds that are pooled postsynthesis to decrease the cost or increase the throughput of screening is fundamentally different from screening compounds that are synthesized as combinatorial mixtures." @default.
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• W1530801019 date "1997-01-01" @default.
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• W1530801019 title "Chapter 26. Discovery and Identification of Lead Compounds from Combinatorial Mixtures" @default.
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• W1530801019 doi "https://doi.org/10.1016/s0065-7743(08)61484-0" @default.
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