在乌吉四组分反应中的多布纳型吡唑并吡啶羧酸
Doebner-type pyrazolopyridine carboxylic acids in an Ugi four-component reaction.
作者信息
Murlykina Maryna V, Kolomiets Oleksandr V, Kornet Maryna M, Sakhno Yana I, Desenko Sergey M, Dyakonenko Victoriya V, Shishkina Svetlana V, Brazhko Oleksandr A, Musatov Vladimir I, Tsygankov Alexander V, Van der Eycken Erik V, 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, 61077, Kharkiv, Ukraine.
出版信息
Beilstein J Org Chem. 2019 Jun 12;15:1281-1288. doi: 10.3762/bjoc.15.126. eCollection 2019.
Substituted 1-pyrazolo[3,4-]pyridine-4- and 1-pyrazolo[3,4-]pyridine-6-carboxamides have been synthetized through a Doebner-Ugi multicomponent reaction sequence in a convergent and versatile manner using diversity generation strategies: combination of two multicomponent reactions and conditions-based divergence strategy. The target products contain as pharmacophores pyrazolopyridine and peptidomimetic moieties with four points of diversity introduced from readily available starting materials including scaffold diversity. A small focused compound library of 23 Ugi products was created and screened for antibacterial activity.
通过Doebner-Ugi多组分反应序列，采用多样性生成策略（两种多组分反应的组合和基于条件的发散策略），以收敛且通用的方式合成了取代的1-吡唑并[3,4-]吡啶-4-甲酰胺和1-吡唑并[3,4-]吡啶-6-甲酰胺。目标产物含有吡唑并吡啶和拟肽部分作为药效基团，从包括骨架多样性在内的易得起始原料引入了四个多样性点。创建了一个由23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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