1255239-54-3

Upstream product

• 1779-10-8 1,6-dibromo-2-hydroxynaphthalene-3-carboxylic acid 
• 92-70-6 3-Hydroxy-2-naphthoic acid 
• 1219689-98-1 7-bromo-3-methoxy-2-naphthaldehyde 
• 1219689-97-0 (7-bromo-3-methoxynaphthalen-2-yl)methanol 
• 123266-51-3 7-bromo-3-methoxynaphthalene-2-carboxylic acid methyl ester 
• 1779-11-9 7-bromo-3-hydroxy-2-naphthoic acid 

Relevant academic research and scientific papers

Design, synthesis and biological evaluation of novel triaryldimethylaminobutan-2-ol derivatives against Mycobacterium tuberculosis

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 BUTAN-2-OL COMPOUNDS, PREPARATION METHODS AND USES THEREOF

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.