773871-34-4

Usage

Classification

Furan carboxylic acid

Structure

Contains a furan ring and a carboxylic acid group, as well as a sulfonamide functional group

Application

Used in the pharmaceutical industry as a building block for the synthesis of various drugs, especially enzyme inhibitors

Properties

Unique structure and properties make it valuable for drug development and medicinal chemistry research

Biological Activity

May exhibit biological activity and has potential applications in the development of new therapeutic agents

Upstream product

• 2527-99-3 methyl 5-bromo-2-furoate 
• 613660-87-0 4-sulfamoylphenylboronic acid 

Relevant academic research and scientific papers

Discovery and development of novel salicylate synthase (MbtI) furanic inhibitors as antitubercular agents

We report on the virtual screening, synthesis, and biological evaluation of new furan derivatives targeting Mycobacterium tuberculosis salicylate synthase (MbtI). A receptor-based virtual screening procedure was applied to screen the Enamine database, identifying two compounds, I and III, endowed with a good enzyme inhibitory activity. Considering the most active compound I as starting point for the development of novel MbtI inhibitors, we obtained new derivatives based on the furan scaffold. Among the SAR performed on this class, compound 1a emerged as the most potent MbtI inhibitor reported to date (Ki = 5.3 μM). Moreover, compound 1a showed a promising antimycobacterial activity (MIC99 = 156 μM), which is conceivably related to mycobactin biosynthesis inhibition.