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 and show comparable efficacy in a mouse model of infection.
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| http://dx.doi.org/10.1039/d4md01004c | DOI Listing |
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Clemastine enhances myelin formation in the striatum and medial prefrontal cortex and improves sociability in a neonatal rat hypoxic-ischemic model.
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Department of Neurology, Medical College of Georgia, Augusta University, 1120 15th Street, Augusta, GA 30912, USA. Electronic address:
Neonatal hypoxia-ischemia (HI) results in gray and white matter injuries, leading to impairments in social behavior and severe neurological deficits. Clemastine treatment has demonstrated efficacy in alleviating behavioral deficits in various neurological disorders by improving myelin formation. It has been suggested that the medial prefrontal cortex (mPFC) and the striatum play a key role in human social behaviors.
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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 and show comparable efficacy in a mouse model of infection.
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