Antibiofilm Activity of a Diverse Oroidin Library Generated through Reductive Acylation

Antibiofilm Activity of a Diverse Oroidin Library Generated through Reductive Acylation
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DOI:
10.1021/jo802260t
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发表时间:
2009-02-20
影响因子:
3.6
通讯作者:
Melander, Christian
Melander, Christian
中科院分区:
化学2区
文献类型:
--
作者:
Ballard, T. Eric;Richards, Justin J.;Melander, Christian

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通过还原酰化策略合成了一个基于海洋生物碱oroidin的不同的20个化合物的类似物库。然后检测最终目标对已知形成生物膜的常见蛋白细菌的抑制和分散活性。这一方法是对已知的含有2-氨基咪唑的底物酰化方法的重大改进,并有可能在合成更先进的oroidin家族成员及其相应的类似物方面具有广泛的应用前景。
A diverse 20-compound library of analogues based on the marine alkaloid oroidin were synthesized via a reductive acylation strategy. The final target was then assayed for inhibition and dispersion activity against common proteo-bacteria known to form biofilms. This methodology represents a significant improvement over the generality of known methods to acylate substrates containing 2-aminoimidazoles and has the potential to have broad application to the synthesis of more advanced oroidin family members and their corresponding analogues.