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

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

doi:10.1021/cc0600270

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

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

PHA - Molecular Pharmaceutical Science

Research output: Contribution to journal › Article › peer-review

33 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 language	English
Pages (from-to)	571-582
Number of pages	12
Journal	Journal of Combinatorial Chemistry
Volume	8
Issue number	4
DOIs	https://doi.org/10.1021/cc0600270
Publication status	Published - 2006 Jul

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10.1021/cc0600270

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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.",

author = "Takayuki Doi and Yoichiro Hoshina and Hiroyuki Mogi and Yoshifumi Yamada and Takashi Takahashi",

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AU - Takahashi, Takashi

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

Abstract

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