%O © 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/
%D 2025
%A Rebecca Charlton
%A Douglas Escrivani
%A Christopher Brown
%A Niranjan Thota
%A Victor de Sousa Agostino
%A Exequiel Porta
%A Timur Avkiran
%A Andrew T Merritt
%A Paul W Denny
%A Bartira Rossi-Bergmann
%A PG Steel
%T Simple Accessible Clemastine Fumarate Analogues as Effective Antileishmanials
%J RSC Medicinal Chemistry
%K Leishmaniasis, Clemastine Fumarate, Inositol Phosphoryl Ceramide Synthase, Enantioselective Synthesis, Drug Discovery
%X 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.
%L discovery10205244
%I Royal Society of Chemistry (RSC)