Identification of cyclic hexapeptides natural products with inhibitory potency against Mycobacterium tuberculosis
oleh: Sheo B. Singh, Joshua Odingo, Mai A. Bailey, Bjorn Sunde, Aaron Korkegian, Theresa O’Malley, Yulia Ovechkina, Thomas R. Ioerger, James C. Sacchettini, Katherine Young, David B. Olsen, Tanya Parish
| Format: | Article |
|---|---|
| Diterbitkan: | BMC 2018-06-01 |
Deskripsi
Abstract Objective Our aim was to identify natural products with anti-tubercular activity. Results A set of ~ 500 purified natural product compounds was screened for inhibition against the human pathogen Mycobacterium tuberculosis. A series of cyclic hexapeptides with anti-tubercular activity was identified. Five analogs from a set of sixteen closely related compounds were active, with minimum inhibitory concentrations ranging from 2.3 to 8.9 μM. Eleven structural analogs had no significant activity (MIC > 20 μM) demonstrating structure activity relationship. Sequencing of resistant mutant isolates failed to identify changes accounting for the resistance phenotype.