1467-70-5Relevant articles and documents
Synthesis of aryl α-keto-acids via the Cu-catalyzed conversion of aryl nitroaldol products
Nikalje, Milind D.,Ali, Iliyas Sayyed,Dewkar, Gajanan K.,Sudalai
, p. 959 - 961 (2000)
Cu(II) salts efficiently catalyze the conversion of a variety of aryl nitroaldol products to afford the corresponding aryl α-keto-acids in high yields using 30% aq. AcOH:MeOH (1:1) as the solvent. (C) 2000 Elsevier Science Ltd.
Novel peptidomimetic peptide deformylase (PDF) inhibitors of Mycobacterium tuberculosis
Gokhale, Kunal M.,Telvekar, Vikas N.
, p. 148 - 156 (2020/08/26)
Emergence of MDR-TB and XDR-TB led to the failure of available anti-tubercular drugs. In order to explore, identify and develop new anti-tubercular drugs, novel peptidomimetic series of Mtb–peptide deformylase (PDF) inhibitors was designed and synthesized. In vitro antimycobacterial potential of compounds was established by screening of compounds against Mycobacterium tuberculosis H37Rv strain using MABA. Among them, ester series of compounds 4a, 4b, 4c, 4d, and 4e were found most active, with compound 4c being highly active and exhibiting minimum inhibitory concentration of 6.25?μg/ml against M.?tb H37Rv strain. Additionally, the compounds were docked to determine the probable binding interactions and understand the mechanism of action of most active molecules on Mtb-peptide deformylase (PDF), which is involved in the mycobacterium protein synthesis.
Rapid assembly of α-ketoamides through a decarboxylative strategy of isocyanates with α-oxocarboxylic acids under mild conditions
Huang, Junjie,Liang, Baihui,Chen, Xiuwen,Liu, Yifu,Li, Yawen,Liang, Jingwen,Zhu, Weidong,Tang, Xiaodong,Li, Yibiao,Zhu, Zhongzhi
supporting information, p. 4783 - 4787 (2021/06/11)
A simple and practical method for α-ketoamide synthesis via a decarboxylative strategy of isocyanates with α-oxocarboxylic acids is described. The reaction proceeds at room temperature under mild conditions without an oxidant or an additive, showing good substrate scope and functional compatibility. Moreover, the applicability of this method was further demonstrated by the synthesis of various bioactive molecules and different application examples through a two-step one-pot operation.
