Solid-phase combinatorial synthesis of aeruginosin derivatives and their biological evaluation.

Journal of combinatorial chemistry

PubMedID: 16827570

Doi T, Hoshina Y, Mogi H, Yamada Y, Takahashi T. Solid-phase combinatorial synthesis of aeruginosin derivatives and their biological evaluation. J Comb Chem. 2006;8(4):571-82.
A 24-member combinatorial library based on the structure of aeruginosin 298-A (1a) was synthesized utilizing solid-phase, and their inhibitory activity against trypsin was evaluated. Among the library, we found that D-Hpla-D-Leu-L-Choi-Agma (1h) is 300 times more potent than the parent natural product 1a.