Gold-Catalyzed Double Cycloisomerization of 1-Ene-4,10-diynyl Esters to Bicyclo[6.3.0]undeca-2,4,9-trienyl Esters.

A synthetic method to prepare bicyclo[6.3.0]undeca-2,4,9,trienyl esters efficiently from gold(I)-catalyzed Rautenstrauch rearrangement/1,5-hydride shift/8-endo-dig cyclization of 1-ene-4,10-diynyl esters is described.

Brønsted Acid-Mediated Cycloaromatization of 1H-Indol-2-yl Propargyl Benzoates to 7H-Benzo[c]carbazoles.

A synthetic method for the efficient assembly of benzo[c]carbazole derivatives that relies on silica gel-activated benzoic acid-mediated cycloaromatization of 1H-indol-2-yl propargyl benzoates under atmospheric conditions is described. Robust with a variety of substitution patterns tolerated, the reaction provides a one-step strategy to construct a member of the N-heterocycles family in good to excellent yields. A tentative mechanism is proposed in which the cycloaromatization process is thought to involve a Brønsted acid-mediated formal 1,3-acyloxy migration/6π-electrocyclization pathway.

Amphiphilic xanthones as a potent chemical entity of anti-mycobacterial agents with membrane-targeting properties.

Tuberculosis (TB) remains a deadly disease and infects one-third of the world's population. Given the low success rates encountered in clinical development, there is an urgent need to identify structurally novel antimicrobials for tuberculosis. The present report details the anti-mycobacterial activities, structure-activity relationships (SARs) and mechanism of action of amphiphilic xanthone derivatives.