In:
International Journal of Molecular Sciences, MDPI AG, Vol. 23, No. 19 ( 2022-10-07), p. 11912-
Kurzfassung:
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.
Materialart:
Online-Ressource
ISSN:
1422-0067
DOI:
10.3390/ijms231911912
Sprache:
Englisch
Verlag:
MDPI AG
Publikationsdatum:
2022
ZDB Id:
2019364-6
SSG:
12
