Abstract
This review describes the recent progress of combinatorial chemistry for drug discovery. Application of combinatorial chemistry is also described to functional studies of biologically active natural products including our studies of bacterial glycoconjugate lipid A. Lipid A analogs were synthesized via a new divergent synthetic route in order to clarify the biological importance of acyl groups. The number and chain length of the fatty acyl groups proved to have crucial influence on the biological activity. The present divergent route opens an efficient way toward the synthesis of lipid A libraries.
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