eprintid: 10205244
rev_number: 7
eprint_status: archive
userid: 699
dir: disk0/10/20/52/44
datestamp: 2025-02-25 13:49:10
lastmod: 2025-02-25 13:49:10
status_changed: 2025-02-25 13:49:10
type: article
metadata_visibility: show
sword_depositor: 699
creators_name: Charlton, Rebecca
creators_name: Escrivani, Douglas
creators_name: Brown, Christopher
creators_name: Thota, Niranjan
creators_name: de Sousa Agostino, Victor
creators_name: Porta, Exequiel
creators_name: Avkiran, Timur
creators_name: Merritt, Andrew T
creators_name: Denny, Paul W
creators_name: Rossi-Bergmann, Bartira
creators_name: Steel, PG
title: Simple Accessible Clemastine Fumarate Analogues as Effective Antileishmanials
ispublished: inpress
divisions: UCL
divisions: B02
divisions: C08
divisions: D10
divisions: G09
keywords: Leishmaniasis, Clemastine Fumarate, Inositol Phosphoryl Ceramide Synthase, Enantioselective Synthesis, Drug Discovery
note: © 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/
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.
date: 2025
date_type: published
publisher: Royal Society of Chemistry (RSC)
official_url: https://doi.org/10.1039/D4MD01004C
oa_status: green
full_text_type: pub
language: eng
primo: open
primo_central: open_green
verified: verified_manual
elements_id: 2364325
doi: 10.1039/D4MD01004C
lyricists_name: Porta, Exequiel
lyricists_id: EPORT93
actors_name: Porta, Exequiel
actors_id: EPORT93
actors_role: owner
full_text_status: public
publication: RSC Medicinal Chemistry
issn: 2632-8682
citation:        Charlton, Rebecca;    Escrivani, Douglas;    Brown, Christopher;    Thota, Niranjan;    de Sousa Agostino, Victor;    Porta, Exequiel;    Avkiran, Timur;                 ... Steel, PG; + view all <#>        Charlton, Rebecca;  Escrivani, Douglas;  Brown, Christopher;  Thota, Niranjan;  de Sousa Agostino, Victor;  Porta, Exequiel;  Avkiran, Timur;  Merritt, Andrew T;  Denny, Paul W;  Rossi-Bergmann, Bartira;  Steel, PG;   - view fewer <#>    (2025)    Simple Accessible Clemastine Fumarate Analogues as Effective Antileishmanials.                   RSC Medicinal Chemistry        10.1039/D4MD01004C <https://doi.org/10.1039/D4MD01004C>.    (In press).    Green open access   
 
document_url: https://discovery.ucl.ac.uk/id/eprint/10205244/1/d4md01004c.pdf