Four new rufomycins, compounds 1-4, named rufomycins 56, 57, 58, and 61, respectively, exhibiting new skeletal features, were obtained from Streptomyces atratus strain MJM3502 and were fully characterized. Compounds 1 and 2 possess a 4-imidazolidinone ring not previously encountered in this family of cyclopeptides, thereby resulting in a [5,17] bicyclic framework. The in vitro anti-Mycobacterium tuberculosis potency of compounds 3 and 4 is remarkable, with minimum inhibitory concentration values of 8.5 and 130 nM, respectively.
Funding
“Targeting Protein Degradation ClpC1 ATPase” | Funder: National Institutes of Health | Grant ID: U19AI142735
History
Citation
Zhou, B., Shetye, G., Wolf, N. M., Chen, S. N., Qader, M., Ray, G. J., Lankin, D. C., Cho, S., Cheng, J., Suh, J. W., Franzblau, S. G., McAlpine, J. B.Pauli, G. F. (2022). New Rufomycins from Streptomyces atratus MJM3502 Expand Anti- Mycobacterium tuberculosis Structure-Activity Relationships. Organic Letters, 24(40), 7265-7270. https://doi.org/10.1021/acs.orglett.2c02493