# Simple accessible clemastine fumarate analogues as effective antileishmanials

**Authors:** Rebecca L. Charlton, Douglas O. Escrivani, Christopher Brown, Niranjan Thota, Victor S. Agostino, Exequiel O. J. Porta, Timur Avkiran, Andrew T. Merritt, Paul W. Denny, Bartira Rossi-Bergmann, Patrick G. Steel

PMC · DOI: 10.1039/d4md01004c · 2025-01-31

## TL;DR

Researchers developed simpler versions of a drug called clemastine fumarate that are easier to make and work well against leishmaniasis.

## Contribution

The study introduces simpler N-linked analogues of clemastine fumarate with improved accessibility and selectivity.

## Key findings

- N-linked analogues are easier to synthesize than clemastine fumarate.
- The analogues show higher selectivity and comparable efficacy in treating Leishmania amazonensis infection in mice.

## 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.

N-linked analogues of clemastine fumarate afford simpler, more accessible, more selective antileishmanials.

## Linked entities

- **Chemicals:** clemastine fumarate (PubChem CID 5281069)
- **Diseases:** leishmaniasis (MONDO:0011989)
- **Species:** Leishmania amazonensis (taxon 5659)

## Full-text entities

- **Diseases:** Leishmania amazonensis infection (MESH:D007896)
- **Species:** Mus musculus (house mouse, species) [taxon 10090]

## Figures

26 figures with captions in the complete paper: https://tomesphere.com/paper/PMC11862611/full.md

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Source: https://tomesphere.com/paper/PMC11862611