1779-11-9Relevant articles and documents
Design, synthesis and biological evaluation of novel triaryldimethylaminobutan-2-ol derivatives against Mycobacterium tuberculosis
Cao, Ruiyuan,Fan, Shiyong,Li, Song,Liu, Ping,Lu, Yu,Wang, Bin,Wang, Xiaokui,Zhong, Wu
, (2020/07/13)
Bedaquiline (TMC207), a typical diarylquinoline anti-tuberculosis drug, has been approved by FDA to specifically treat MDR-TB. Herein we describe design, synthesis, and in vitro biological evaluation against Mycobacterium tuberculosis of a series of triaryldimethylaminobutan-2-ol derivatives obtaining from the structural modification of TMC207. Compounds 23, 25, 28, 32, 39 and 43 provided superior anti-mycobacterial activity than positive control PC01 which shows the same configuration and contains TMC207. Compounds 16, 20, 29, 34, 37, 45 and 47 exhibited the similar activity to positive control PC01. Most importantly, the series of compounds showed excellent activity against XDR-Mtb. The result of acute toxicity suggested that this class of triaryldimethylaminobutan-2-ol derivatives should be graded as low. Further SAR analysis indicates that a large steric bulk of triaryl and 7-Br, 3-OCH3 on 1-naphthyl are critical.
Hydrazide derivatives and application thereof
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Paragraph 0193; 0194, (2018/08/28)
The invention provides hydrazide derivatives and pharmaceutically acceptable salts thereof obtained through chemical synthesis. Pharmacological experiments prove that the compounds have the activity of resisting tumor cell proliferation, part of the compounds show the activity of inhibiting dimerization of protein DJ-1, and the compounds can be used for preparing drugs for treating, preventing andinhibiting DJ-1-associated tumor, type 2 diabetes as well as neurodegenerative diseases such as Parkinson s disease, Alzheimer's disease and the like. The general structural formula I of the compounds is shown in the description.
Asymmetric synthesis and absolute configuration assignment of a new type of bedaquiline analogue
Qiao, Chang-Jiang,Wang, Xiao-Kui,Xie, Fei,Zhong, Wu,Li, Song,Dehaen, Wim
, p. 22272 - 22285 (2016/01/25)
Bedaquiline is the first FDA-approved new chemical entity to fight multidrug-resistant tuberculosis in the last forty years. Our group replaced the quinoline ring with a naphthalene ring, leading to a new type of triarylbutanol skeleton. An asymmetric synthetic route was established for our bedaquiline analogues, and the goal of assigning their absolute configurations was achieved by comparison of experimental and calculated electronic circular dichroism spectra, and was confirmed by the combined use of circular dichroism and NMR spectroscopy.
