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Solid-Phase Organic Synthesis. Edited by Kevin Burgess Copyright © 2000 John Wiley & Sons, Inc. ISBNs: 0-471-31825-6 (Hardback); 0-471-22824-9 (Electronic)
82 BENZOFUSED HETEROCYCLES VIA SOLID-PHASE SWAR REACTIONS
In drug discovery there are principally two useful library formats. The first may be called “primary libraries” for use in high-throughput screening, where a priori no specific structure or substructure is obligatory as a starting point. Conversely, “focused (or biased) libraries” are purposefully constructed around a known starting structure having biological activity, to be used in optimizing the activity (or other properties) of the lead compound.
Our group has recently been particularly interested in primary libraries from which pharmaceutically attractive lead molecules might hopefully be found. One goal has been to assemble a portfolio of small-molecule libraries to be used in initial lead discovery against a broad panel of emerging and proven pharmaceutical targets. Relying exclusively on solid-phase methods, we have tried to achieve a blend between generating (i) scaffolds with proven pedigree in medicinal chemistry (e.g., (3-lactams, benzodiazepines);
(ii) other templates densely packed with functional groups that have received less systematic investigation; and (iii) “novel,” unexplored chemo-types. Among questions of significant interest are the relative merits of screening numerous libraries of moderate size (say 10,000-50,000 members) comprising many different template structures, versus screening numerically larger libraries (>>100,000 members) of a limited selection of chemotypes.