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

Takayuki Doi, Yoichiro Hoshina, Hiroyuki Mogi, Yoshifumi Yamada, Takashi Takahashi

Research output: Contribution to journalArticlepeer-review

30 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)571-582
Number of pages12
JournalJournal of Combinatorial Chemistry
Volume8
Issue number4
DOIs
Publication statusPublished - 2006 Jul
Externally publishedYes

ASJC Scopus subject areas

  • Chemistry(all)

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