通过格罗布克-布莱克本-比纳梅反应和乌吉反应串联合成含咪唑并[1,2 - ]吡啶的拟肽
Synthesis of imidazo[1,2-]pyridine-containing peptidomimetics by tandem of Groebke-Blackburn-Bienaymé and Ugi reactions.
作者信息
Kolomiiets Oleksandr V, Tsygankov Alexander V, Kornet Maryna N, Brazhko Aleksander A, Musatov Vladimir I, Chebanov Valentyn A
机构信息
Division of Chemistry of Functional Materials, State Scientific Institution "Institute for Single Crystals" of National Academy of Sciences of Ukraine, Nauky Ave., 60, 61072, Kharkiv, Ukraine.
Faculty of Chemistry, V. N. Karazin Kharkiv National University, Svobody sq., 4, 61022, Kharkiv, Ukraine.
出版信息
Beilstein J Org Chem. 2023 May 26;19:727-735. doi: 10.3762/bjoc.19.53. eCollection 2023.
Peptidomimetics with a substituted imidazo[1,2-]pyridine fragment were synthesized by a tandem of Groebke-Blackburn-Bienaymé and Ugi reactions. The target products contain substituted imidazo[1,2-]pyridine and peptidomimetic moieties as pharmacophores with four diversity points introduced from readily available starting materials, including scaffold diversity. A small focused compound library of 20 Ugi products was prepared and screened for antibacterial activity.
通过Groebke-Blackburn-Bienaymé反应与Ugi反应串联，合成了带有取代咪唑并[1,2 -]吡啶片段的拟肽。目标产物含有取代咪唑并[1,2 -]吡啶和拟肽部分作为药效基团，从容易获得的起始原料引入了四个多样性点，包括骨架多样性。制备了一个由20种Ugi产物组成的小型聚焦化合物库，并对其进行抗菌活性筛选。
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