Chemical, Biochemical, Cellular, and Physiological Characterization of Leucettinib-21, a Down Syndrome and Alzheimer's Disease Drug Candidate.

Leucettinibs are substituted 2-aminoimidazolin-4-ones (inspired by the marine sponge natural product Leucettamine B) developed as pharmacological inhibitors of DYRK1A (dual-specificity, tyrosine phosphorylation-regulated kinase 1A), a therapeutic target for indications such as Down syndrome and Alzheimer's disease. Leucettinib-21 was selected as a drug candidate following extensive structure/activity studies and multiparametric evaluations. We here report its physicochemical properties (X-ray powder diffraction, differential scanning calorimetry, stability, solubility, crystal structure) and drug-like profile.

Ordered and Disordered Carboxylic Acid Monolayers on Calcite (104) and Muscovite (001) Surfaces.

The adsorption of carboxylic acid molecules at the calcite (104) and the muscovite (001) surface was investigated using surface X-ray diffraction. All four investigated carboxylic acid molecules, hexanoic acid, octanoic acid, lauric acid, and stearic acid, were found to adsorb at the calcite surface. Whereas the shortest two carboxylic acid molecules, hexanoic acid and octanoic acid, showed limited ordering and a flexible, disordered chain, the two longest carboxylic acid molecules form fully ordered monolayers, i.

Epitaxy of Rhodochrosite (MnCO) on Muscovite Mica and Its Relation with Calcite (CaCO).

The flatness of muscovite mica makes it a convenient substrate to study epitaxy. We have analyzed the growth of rhodochrosite (MnCO) crystals in solution and on muscovite mica. Growth at high supersaturations occurs via the formation of amorphous MnCO, which over time transforms into the crystalline form.

Organothiol Monolayer Formation Directly on Muscovite Mica.

Organothiol monolayers on metal substrates (Au, Ag, Cu) and their use in a wide variety of applications have been extensively studied. Here, the growth of layers of organothiols directly onto muscovite mica is demonstrated using a simple procedure. Atomic force microscopy, surface X-ray diffraction, and vibrational sum-frequency generation IR spectroscopy studies revealed that organothiols with various functional endgroups could be self-assembled into (water) stable and adaptable ultra-flat organothiol monolayers over homogenous areas as large as 1 cm .

Monovalent - divalent cation competition at the muscovite mica surface: Experiment and theory.

Hypothesis: Ion adsorption on mineral surfaces depends on several factors, such as the mineral surface structure and the valency, size and hydration of the ion. In order to understand competitive adsorption at mineral surfaces, experimental techniques are required that can probe multiple ionic species at the same time. By comparing adsorption of two different cations, it should be possible to derive the factors governing ion adsorption.

The crystal structures of four di-meth-oxy-benzaldehyde isomers.

The crystal structures of four di-meth-oxy-benzaldehyde (CHO) isomers, namely the 2,3-, 2,4-, 2,5- and 3,5- isomers, are reported and compared to the previously reported crystal structures of 3,4-di-meth-oxy-benzaldehyde and 2,6-di-meth-oxy-benzaldehyde. All di-meth-oxy-benzaldehyde mol-ecules in the crystal structures are nearly planar. The largest deviation (1.

The structure of PbCl on the {100} surface of NaCl and its consequences for crystal growth.

The role that additives play in the growth of sodium chloride is a topic which has been widely researched but not always fully understood at an atomic level. Lead chloride (PbCl) is one such additive which has been reported to have growth inhibition effects on NaCl {100} and {111}; however, no definitive evidence has been reported which details the mechanism of this interaction. In this investigation, we used the technique of surface x-ray diffraction to determine the interaction between PbCl and NaCl {100} and the structure at the surface.

Concentration-Dependent Adsorption of CsI at the Muscovite-Electrolyte Interface.

The interfacial structure of muscovite in contact with aqueous CsI solutions was measured using surface X-ray diffraction for several CsI concentrations (2-1000 mM). At CsI concentrations up to 200 mM, Cs adsorption is likely hindered by HO, as both cations compete for the adsorption site above the muscovite hexagonal cavity. Above this concentration, more Cs adsorbs than is required to compensate the negatively charged muscovite surface, which means that coadsorption of an anion takes place.

Do solid-to-solid polymorphic transitions in DL-norleucine proceed through nucleation?

DL-Norleucine is a molecular crystal exhibiting two enantiotropic phase transitions. The high temperature α ↔ γ transition has been shown to proceed through nucleation and growth [Mnyukh et al., J.