TY  - INPR
Y1  - 2025///
AV  - public
TI  - Simple Accessible Clemastine Fumarate Analogues as Effective Antileishmanials
N1  - © 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/
PB  - Royal Society of Chemistry (RSC)
UR  - https://doi.org/10.1039/D4MD01004C
SN  - 2632-8682
N2  - 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.
ID  - discovery10205244
A1  - Charlton, Rebecca
A1  - Escrivani, Douglas
A1  - Brown, Christopher
A1  - Thota, Niranjan
A1  - de Sousa Agostino, Victor
A1  - Porta, Exequiel
A1  - Avkiran, Timur
A1  - Merritt, Andrew T
A1  - Denny, Paul W
A1  - Rossi-Bergmann, Bartira
A1  - Steel, PG
KW  - Leishmaniasis
KW  -  Clemastine Fumarate
KW  -  Inositol Phosphoryl Ceramide Synthase
KW  -  Enantioselective Synthesis
KW  -  Drug Discovery
JF  - RSC Medicinal Chemistry
ER  -