Abstract
In the present study, we report four new dihydro-β-agarofuran sesquiterpenes ( 1– 4), which were isolated from the leaves of Celastrus vulcanicola, in addition to five derivatives ( 5– 9). Their stereostructures were elucidated on the basis of spectroscopic analysis, including 1D and 2D NMR techniques, X-ray studies, chemical correlations and biogenetic means. Compounds 1– 9 and the previously reported sesquiterpenes 10– 25 have been tested as potential antimycobacterial agents against sensitive and resistant Mycobacterium tuberculosis strains. 1α-Acetoxy-6β,9β-dibenzoyloxy-dihydro-β-agarofuran ( 20) exhibited antituberculosis activity against the MDR TB strain with a MIC value of 6.2 μg/mL, comparable to or better than isoniazid or rifampin, two of the best first-line drugs commonly used in the treatment of TB. The structure–activity relationship is discussed.
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