| ZFIN ID: ZDB-PUB-180321-28 |
Anti-Tubercular bis-Substituted Cyclam Derivatives: Structure-Activity Relationships and In Vivo Studies
Spain, M., Wong, J.K., Nagalingam, G., Batten, J.M., Hortle, E., Oehlers, S., Jiang, X.F., Murage, H.E., Orford, J.T., Crisologo, P., Triccas, J.A., Rutledge, P.J., Todd, M.H.
| Date: | 2018 |
|---|---|
| Source: | Journal of medicinal chemistry 61(8): 3595-3608 (Journal) |
| Registered Authors: | Hortle, Elinor, Oehlers, Stefan |
| Keywords: | none |
| MeSH Terms: |
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| PubMed: | 29558124 Full text @ J. Med. Chem. |
Citation
Spain, M., Wong, J.K., Nagalingam, G., Batten, J.M., Hortle, E., Oehlers, S., Jiang, X.F., Murage, H.E., Orford, J.T., Crisologo, P., Triccas, J.A., Rutledge, P.J., Todd, M.H. (2018) Anti-Tubercular bis-Substituted Cyclam Derivatives: Structure-Activity Relationships and In Vivo Studies. Journal of medicinal chemistry. 61(8):3595-3608.
ABSTRACT
We recently reported the discovery of non-toxic cyclam-derived compounds that are active against drug-resistant Mycobacterium tuberculosis. In this paper we report exploration of the structure-activity relationship for this class of compounds, identifying several simpler compounds with comparable activity. The most promising compound identified, possessing significantly improved water solubility, displayed high levels of bacterial clearance in an in vivo zebrafish embryo model, suggesting this compound series has promise for in vivo treatment of tuberculosis.
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