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 and Patrick G. Steel
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Simple accessible clemastine fumarate analogues as effective antileishmanials†
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.
期刊介绍:
Research and review articles in medicinal chemistry and related drug discovery science; the official journal of the European Federation for Medicinal Chemistry.
In 2020, MedChemComm will change its name to RSC Medicinal Chemistry. Issue 12, 2019 will be the last issue as MedChemComm.