Charlton, Rebecca;
Escrivani, Douglas;
Brown, Christopher;
Thota, Niranjan;
de Sousa Agostino, Victor;
Porta, Exequiel;
Avkiran, Timur;
... Steel, PG; + view all
(2025)
Simple Accessible Clemastine Fumarate Analogues as Effective Antileishmanials.
RSC Medicinal Chemistry
10.1039/D4MD01004C.
(In press).
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Abstract
Current therapeutic options for leishmaniasis are severely limited, highlighting an urgent need to develop more effective and less toxic drugs to combat a major global public health challenge. Clemastine fumarate displays good levels of antileishmanial efficacy, but further optimisation is challenged by its difficult synthesis. Here, we demonstrate that simple N-linked analogues are easier to access, can exhibit higher selectivity and show comparable efficacy in a mouse model of Leishmania amazonensis infection.
| Type: | Article |
|---|---|
| Title: | Simple Accessible Clemastine Fumarate Analogues as Effective Antileishmanials |
| Open access status: | An open access version is available from UCL Discovery |
| DOI: | 10.1039/D4MD01004C |
| Publisher version: | https://doi.org/10.1039/D4MD01004C |
| Language: | English |
| Additional information: | © The Author(s), 2025. This is an Open Access article distributed under the terms of the Creative Commons Attribution Licence (CC BY 3.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. https://creativecommons.org/licenses/by/3.0/ |
| Keywords: | Leishmaniasis, Clemastine Fumarate, Inositol Phosphoryl Ceramide Synthase, Enantioselective Synthesis, Drug Discovery |
| UCL classification: | UCL UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy > Pharma and Bio Chemistry |
| URI: | https://discovery.ucl.ac.uk/id/eprint/10205244 |
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