1779-10-8Relevant 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.
Aromatic 2-butanol chiral compound, asymmetric synthesis and medical application of aromatic 2-butanol chiral compound
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Paragraph 0075; 0076; 0077, (2017/08/29)
The invention relates to an aromatic 2-butanol chiral compound, a chiral synthetic method and a medical application of the aromatic 2-butanol chiral compound. The aromatic 2-butanol chiral compound has a chemical structure of the general formula I, contains two chiral centers, and is prepared through 18-step reaction. In the reaction, the optical purity of the final product is decided through the Sharpless asymmetric epoxidation step. Compared with the method in the prior art, the method allows four optical isomers of the compound with the general formula I to be conveniently prepared, and the enantioselectivity is high (the e.e. value can reach 87-97%). The invention further relates to the compound, pharmaceutically acceptable salt and solvate thereof, and an application of a pharmaceutical composition containing the compound to prevent or treat diseases or symptoms related to mycobacterium tuberculosis infection.
AROMATIC BUTAN-2-OL COMPOUNDS, PREPARATION METHODS AND USES THEREOF
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Paragraph 0051; 0052, (2013/04/10)
The present invention relates to aromatic butan-2-ol compounds and preparation methods and uses thereof. Specifically, the present invention relates to the compound of Formula I, or an optical isomer, racemate, diastereomer, pharmaceutically acceptable salt or solvate thereof: wherein each of the substituents have the definitions as given in the specification. The present invention further relates to a pharmaceutical composition containing the compound, and the use of the compound in manufacture of a medicament for the treatment and/or prophylaxis of a disease or disorder caused by tubercle bacillus infection. The compound of Formula I of the present invention has advantages in treatment and/or prophylaxis of a disease or disorder caused by tubercle bacillus infection.