51925-56-5Relevant articles and documents
Structure-activity relationship study of 3-amino-2-indolyllactam derivatives: Development of inhibitors of oxidative stress-induced necrosis
Dodo, Kosuke,Hayamizu, Kenji,Shimizu, Tadashi,Sodeoka, Mikiko
, p. 886 - 898 (2016)
Modification of our previously reported selective inhibitor of oxidative stress-induced necrosis, 2-(1H-indol-3-yl)-3-pentylamino-maleimide (IM-54) by regioselective reduction of the C-4 carbonyl group afforded a 3-amino-2-indolyllactam (IL-1) with more potent activity. To examine the structure-activity relationship of IL derivatives, we developed new synthetic routes with flexibility to incorporate a range of substituents at a late stage. The synthesized IL derivatives were evaluated for activity to inhibit necrotic cell death induced by hydrogen peroxide. Among them, IL-12 showed the most potent activity (IC50=49 nM) among the IL and indolylmaleimide (IM) derivatives examined.
Studies on the synthesis and bioactivities of 4-amino derivatives of tetramic acid
Liu, Yu-Xiu,Zhao, Hua-Ping,Song, Hai-Bin,Gu, Yu-Cheng,Wang, Qing-Min
, p. E25-E33 (2014/11/07)
In order to study the potential bioactivities of 4-amino tetramic acid derivatives, the 4-amination products of pyrrolidine-2,4-diones (5) and 4-hydroxy-2-oxo-2,5-dihydro-1H-pyrrole-3-carboxylates (4) were prepared. The 4-amination of 5 took place in high yield when catalyzed by acetic acid, whereas the 4-amination of 4 was achieved through a 4-ethoxy intermediate, which was prepared by acidic etherification. Their herbicidal, fungicidal, insecticidal, and antitumor activities were tested. The bioassays showed that two of the compounds exhibited good herbicidal activity against dicot Arabidopsis thaliana at a concentration of 10 μg/mL, and one compound gave instinct fungicidal activity against Pythium sp. at a concentration of 2 μg/mL.
Tetramic acids as scaffolds: Synthesis, tautomeric and antibacterial behaviour
Jeong, Yong-Chul,Moloney, Mark G.
scheme or table, p. 2487 - 2491 (2010/03/01)
Efficient synthetic routes for tetramic acids variously substituted on the ring nitrogen, their tautomeric behaviour in solution and their antibiotic activity are reported.