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 and show comparable efficacy in a mouse model of infection.

Catalysis-driven Active Transport Across a Liquid Membrane.

Biology has mastered energy transduction, converting energy between various forms, and employing it to drive its vital processes. Central to this is the ability to use chemical energy for the active transport of substances, pumping ions and molecules across hydrophobic lipid membranes between aqueous (sub)cellular compartments. Biology employs information ratchet mechanisms, where kinetic asymmetry in the fuel-to-waste (i.

A guide to bullvalene stereodynamics.

Here, we analyze the stereodynamic properties of bullvalenes using principal moments of inertia and exit vector plots to draw comparisons with commonly used ring systems in medicinal chemistry. To aid analyses, we first classify (i) the four elementary rearrangement steps available to substituted bullvalenes, which (ii) can be described by applying positional descriptors (α, β, γ, and δ) to the substituents. We also (iii) derive an intuitive equation to calculate the number of isomers for a given bullvalene system.

π-Expanded Thioxanthones - Engineering the Triplet Level of Thioxanthone Sensitizers for Lanthanide-Based Luminescent Probes with Visible Excitation.

Bright lanthanide based probes for optical bioimaging must rely on the antenna principle, where the lanthanide-centred excited state is formed by a complex sensitization process. Efficient sensitization of lanthanide-centred emission occurs via triplet states centred on the sensitizing chromophore. Here, the triplet state of thioxanthone chromophores is modulated by extending the π-system.

Effect of terminal chain length on the helical twisting power in achiral bent-core molecules doped in a cholesteric liquid crystal.

We prepared a homologous series of achiral bent-core (BC) liquid crystals with different terminal alkoxy chain lengths, (BC-), and evaluated the helical twisting power (HTP) of the BC- doped in a cholesteric liquid crystal. The BC- molecules with longer terminal chains showed larger HTPs. To interpret this striking phenomenon, a stochastic dynamics simulation was performed to determine the distribution of the chirality order parameters () for BC molecules with = 8-16.