Antimycobacterial Rufomycin Analogues from Streptomyces atratus Strain MJM3502
2020
This study represents a systematic
chemical and biological study
of the rufomycin (RUF) class of cyclic heptapeptides, which our anti-TB
drug discovery efforts have identified as potentially promising anti-TB
agents that newly target the caseinolytic protein C1, ClpC1. Eight
new RUF analogues, rufomycins NBZ1–NBZ8 (1–8), as well as five known peptides (9–13) were isolated and characterized from the Streptomyces
atratus strain MJM3502. Advanced Marfey’s and X-ray
crystallographic analysis led to the assignment of the absolute configuration
of the RUFs. Several isolates exhibited potent activity against both
pathogens M. tuberculosis H37Rv and M. abscessus, paired with favorable selectivity (selectivity index >60), which
collectively underscores the promise of the rufomycins as potential
anti-TB drug leads.
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