Combinatorial chemistry: Libraries from libraries, the art of the diversity-oriented transformation of resin-bound peptides and chiral polyamides to low molecular weight acyclic and heterocyclic compounds

被引:98
作者
Nefzi, A [1 ]
Ostresh, JM [1 ]
Yu, JP [1 ]
Houghten, RA [1 ]
机构
[1] Torrey Pines Inst Mol Studies, San Diego, CA 92121 USA
关键词
D O I
10.1021/jo040114j
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Combinatorial chemistry has deeply impacted the drug discovery process by accelerating the synthesis and screening of large numbers of compounds having therapeutic and/or diagnostic potential. These techniques offer unique enhancement in the potential identification of new and/or therapeutic candidates. Our efforts over the past 10 years in the design and diversity-oriented synthesis of low molecular weight acyclic and heterocyclic combinatorial libraries derived from amino acids, peptides, and/or peptidomimetics are described. Employing a "toolbox" of various chemical transformations, including alkylation, oxidation, reduction, acylation, and the use of a variety of multifunctional reagents, the "libraries from libraries" concept has enabled the continued development of an ever-expanding, structurally varied series of organic chemical libraries.
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收藏
页码:3603 / 3609
页数:7
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