Kozmenko Yaroslav V, Khisamov Marat M, Revtovich Svetlana V, Korolev Sergey P, Sherman Daria K, Spiridonov Vasiliy V, Kalnina Lyudmila B, Valuev-Elliston Vladimir T, Gottikh Marina B, Kochetkov Sergey N, Zemskaya Anastasia S, Solyev Pavel N
Engelhardt Institute of Molecular Biology, Moscow 119991, Russia.
Chemistry Department, Lomonosov Moscow State University, Moscow 119992, Russia.
Int J Mol Sci. 2025 Aug 29;26(17):8402. doi: 10.3390/ijms26178402.
Aromatic hydrazones of 7-hydrazino-8-hydroxyquinoline were studied as anti-HIV and antibacterial compounds. A set of the compounds with different aromatic moieties bearing electron-donating and electron-withdrawing substituents has been selected and obtained via the hydrazo coupling and "one-pot" click reaction with aldehydes. The compounds possess activity against both bacterial and fungal targets. Cellular Ku70-inhibiting activity has been found for the series, opening a new class of inhibitors for potential anti-HIV treatment. The compounds display anti-HIV activity in infected cells at submicromolar concentrations. Their low solubility can be overcome by incorporation in water-soluble neutral polyalginate microgels (33% wt load of the compound).
对7-肼基-8-羟基喹啉的芳香腙作为抗HIV和抗菌化合物进行了研究。通过肼偶联和与醛的“一锅法”点击反应，选择并获得了一组带有供电子和吸电子取代基的不同芳香部分的化合物。这些化合物对细菌和真菌靶点均具有活性。已发现该系列化合物具有细胞Ku70抑制活性，为潜在的抗HIV治疗开辟了一类新的抑制剂。这些化合物在亚微摩尔浓度下对受感染细胞显示出抗HIV活性。通过将其掺入水溶性中性海藻酸盐微凝胶中（化合物的重量负载量为33%），可以克服它们的低溶解度。
