AI Article Synopsis
- Simplified versions of a bacterial-specific molecule called mycothiol were created to potentially deliver antimycobacterial drugs effectively.
- Initial tests showed these mycothiol analogues had promising effects against model Mycobacteria, but more work is needed to enhance their targeting ability.
Article Abstract
Drug-resistant Mycobacterium tuberculosis is a growing health problem. As proof of principle that the bacterial-specific metabolite mycothiol could be used as a delivery agent for antimycobacterial agents, simplified analogues of mycothiol were synthesised containing an S-trichloroethenyl substituted cysteine residue. It was envisaged that uptake of the mycothiol analogue would be followed by release of the known cytotoxin S-trichloroethenyl cysteine by the action of mycothiol S-conjugate amidase or its paralog, mycothiol deacetylase MshB. Promising activity was displayed against model Mycobacteria, although further development will be required to improve selectivity.
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| http://dx.doi.org/10.1016/j.bmcl.2015.03.070 | DOI Listing |
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