engleski

Novel linear diamine disubstituted polycyclic ‘cage’ derivatives as potential anti-mycobacterial candidates

As part of an ongoing project to develop highly potent anti-tuberculosis therapeutics, a series novel polycyclic ‘cage’ tetra-amines were synthesized and screened for in-vitro antituberculosis activities against the H37Rv strain of tuberculosis. Three disubstituted polycyclic moieties, namely pentacyclodecane, pentacycloundecane (PCU), and tricyclodecane were used in this study. Compounds 5 and 7 showed similar activity to SQ109 at a MIC of 1 μM while compounds 4, 6 and 8 displayed MIC activity at 1<MIC<10 μM. This study demonstrates the first reported analysis of pentacyclo[5.3.0.02, 5.03, 9.04, 8]decane as a potential therapeutic agent.

anti-tuberculosis activity; SQ109; pentacyclodecane; pentacycloundecane and tricyclodecane; isoprenyl diamine

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