微波辅助抗菌二肽类化合物的固相合成
Microwave-Facilitated SPOT-Synthesis of Antibacterial Dipeptoids.
作者信息
Schneider Anne C, Fritz Daniel, Vasquez Joseph K, Vollrath Sidonie B L, Blackwell Helen E, Bräse Stefan
机构信息
Institute of Organic Chemistry, Karlsruhe Institute of Technology , Fritz-Haber-Weg 6, 76131 Karlsruhe, Germany.
Department of Chemistry, University of Wisconsin-Madison , 1101 University Avenue, Madison, Wisconsin 53706, United States.
出版信息
ACS Comb Sci. 2017 Dec 11;19(12):715-737. doi: 10.1021/acscombsci.7b00096. Epub 2017 Nov 7.
With microwave irradiation, the submonomer synthesis of dipeptoids on functionalized cellulose can be accelerated with good yields and purity. Optimization provided a library of 96 dipeptoids. From these, 29 compounds were found with an antibacterial activity against MRSA at a concentration of 25 μM. Large nonpolar residues, such as undecylamine and dehydroabiethylamine, are the key components engendering the observed antibacterial activity of these peptoids.
通过微波辐射，功能化纤维素上二肽类化合物的亚单体合成可以加速，产率和纯度良好。优化后得到了一个包含96种二肽类化合物的文库。从中发现，有29种化合物在浓度为25μM时对耐甲氧西林金黄色葡萄球菌（MRSA）具有抗菌活性。大的非极性残基，如十一胺和脱氢松香乙胺，是导致这些肽类化合物具有所观察到的抗菌活性的关键成分。
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