期刊
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
卷 23, 期 19, 页码 -出版社
MDPI
DOI: 10.3390/ijms231911912
关键词
leishmaniasis; minor groove binders; S-MGB; DNA
资金
- EPSTC DTP award [EP/T517938/1 (2432483)]
- Wellcome Trust [210103/A/18/Z]
- UKRI FLF [MR/T020970/1]
The study found that Strathclyde minor groove binders (S-MGBs) have potent activity against Leishmania parasites, and modification of the tertiary amine tail with an N-oxide derivative can lead to selective anti-leishmanial activity. The findings suggest that S-MGBs can be further studied as novel therapeutics for the treatment of leishmaniasis.
The neglected tropical disease leishmaniasis, caused by Leishmania spp., is becoming more problematic due to the emergence of drug-resistant strains. Therefore, new drugs to treat leishmaniasis, with novel mechanisms of action, are urgently required. Strathclyde minor groove binders (S-MGBs) are an emerging class of anti-infective agent that have been shown to have potent activity against various bacteria, viruses, fungi and parasites. Herein, it is shown that S-MGBs have potent activity against L. donovani, and that an N-oxide derivation of the tertiary amine tail of typical S-MGBs leads to selective anti-leishmanial activity. Additionally, using S-MGB-219, the N-oxide derivation is shown to retain strong binding to DNA as a 2:1 dimer. These findings support the further study of anti-leishmanial S-MGBs as novel therapeutics.
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