Literature DB >> 16827570

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

Takayuki Doi1, Yoichiro Hoshina, Hiroyuki Mogi, Yoshifumi Yamada, Takashi Takahashi.   

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.

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Year:  2006        PMID: 16827570     DOI: 10.1021/cc0600270

Source DB:  PubMed          Journal:  J Comb Chem        ISSN: 1520-4766


  2 in total

1.  Synthesis of hydroxylated bicyclic amino acids from L-tyrosine: octahydro-1H-indole carboxylates.

Authors:  Joshua G Pierce; Dhanalakshmi Kasi; Makoto Fushimi; Anthony Cuzzupe; Peter Wipf
Journal:  J Org Chem       Date:  2008-09-04       Impact factor: 4.354

2.  Total synthesis of aeruginosin 98B.

Authors:  Barry M Trost; Toshiyuki Kaneko; Neil G Andersen; Christoph Tappertzhofen; Bruce Fahr
Journal:  J Am Chem Soc       Date:  2012-11-12       Impact factor: 15.419

  2 in total

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