History of Combinatorial Chemistry

Combinatorial chemistry was first conceived about 15 years ago - although it wasn't called that until the early 1990s. Initially, the field focused primarily on the synthesis of peptide and oligonucleotide libraries. H. Mario Geysen, distinguished research scientist at Glaxo Wellcome Inc., Research Triangle Park, N.C., helped jump-start the field in 1984 when his group developed a technique for synthesizing peptides on pin-shaped solid supports. At the Coronado conference, Geysen reported on his group's recent development of an encoding strategy in which molecular tags are attached to beads or linker groups used in solid-phase synthesis. After the products have been assayed, the tags are cleaved and determined by mass spectrometry (MS) to identify potential lead compounds.

Although combinatorial chemistry has only really been taken up by industry since the 1990s, its roots can be seen as far back as the 1960s when a researcher at Rockefeller University, Bruce Merrifield, started investigating the solid-state synthesis of peptides.

In the past decade there has been a lot of research and development in combinatorial chemistry applied to the discovery of new compounds and materials. This work was pioneered by P.G. Schultz et al. in the mid nineties (Science, 1995, 268: 1738-1740) in the context of luminescent materials obtained by co-deposition of elements on a silicon substrate. Since then the work has been pioneered by several academic groups as well as industries with large R&D programs (Symyx Technologies, GE, etc).

See also the following links: Short description of history of development of combinatorial chemistry

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