Abstract
6-Hydroxy-2-methylbenzofuran-4-carboxylic acid was synthesized in two steps, starting from 3,5-dihydroxybenzoate. The product was obtained through a direct thermal one-pot cyclization with propargyl bromide, followed by a base-catalyzed hydrolysis. Its molecular structure was elucidated by means of mono- and bidimensional NMR techniques, ESI-MS, FT-IR and single-crystal X-ray diffraction.
Highlights
Tuberculosis (TB) is a contagious and virulent disease, mainly caused by the pathogenMycobacterium tuberculosis (Mtb); despite having afflicted mankind for centuries, it is still responsible for thousands of deaths in developed and developing countries [1]
With the purpose of synthesizing structurally simplified analogs of compound I that were devoid of the carbonyl function at position 4 and of the methyl group in 2, we unexpectedly isolated a new benzofuran derivative (1), which was submitted to a complete chemical characterization and tested against MbtI
With and the of synthesizing structurally simplified analogs of compound I that were devoid of the carbonyl function at position 4 and ofacid the methyl in 2, weby unexpectedly isolated
Summary
Tuberculosis (TB) is a contagious and virulent disease, mainly caused by the pathogen. Our attention has been turned to the identification of new inhibitors of the salicylate synthase MbtI, an essential, mycobacterium-specific enzyme involved in iron acquisition [7,8,9,10]. In this context, the chromanone nucleus caught our attention: new compounds bearing the chromane scaffold were synthetized [11], and their biological evaluation allowed the identification of I (Figure 1).
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