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.
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.
Nefzi
Adel
A
Torrey Pines Institute for Molecular Studies, 3550 General Atomics Court, San Diego, California 92121, USA.
Ostresh
John M
JM
Yu
Yongping
Y
Yu
Jongping
J
Houghten
Richard A
RA
D000596:Amino Acids / Q000737:chemistry; D020650:Combinatorial Chemistry Techniques; D006571:Heterocyclic Compounds / Q000737:chemistry*; D006839:Hydrocarbons, Acyclic / Q000737:chemistry*; D015394:Molecular Structure; D008970:Molecular Weight; D009757:Nylons / Q000737:chemistry*; D019151:Peptide Library; D010455:Peptides / Q000737:chemistry*; D012117:Resins, Synthetic
D000596:Amino Acids; D006571:Heterocyclic Compounds; D006839:Hydrocarbons, Acyclic; D009757:Nylons; D019151:Peptide Library; D010455:Peptides; D012117:Resins, Synthetic