Department of Bioorganic Chemistry, Leibniz Institute of Plant Biochemistry, Weinberg 3, D-06120 Halle/Saale, Germany.
Beilstein J Org Chem. 2015 Jan 7;11:25-30. doi: 10.3762/bjoc.11.4. eCollection 2015.
A library of ten 1,3-diyne-linked peptoids has been synthesized through an Ugi four-component reaction (U-4CR) followed by a copper-catalysed alkyne homocoupling (Glaser reaction). The short and chemoselective reaction sequence allows generating diverse (pseudo) dimeric peptoids. A combinatorial version allows the one-pot preparation of, e.g., six-compound-libraries of homo- and heterodimers verified by ESI-MS and HPLC. In a preliminary evaluation, some compounds display moderate activity against the Gram-positive bacterium Bacillus subtilis.
已经通过 Ugi 四组分反应（U-4CR）和铜催化的炔烃偶联（Glaser 反应）合成了一个包含十个 1,3-二炔基连接的肽的库。这种简短且选择性的反应序列允许生成多样化的（拟）二聚肽。组合版本允许一锅法制备例如同二聚体和异二聚体的六化合物文库，通过 ESI-MS 和 HPLC 进行验证。在初步评估中，一些化合物对革兰氏阳性菌枯草芽孢杆菌显示出中等的活性。
