Complexation Thermodynamics of Cyclodextrins.

This report describes a number of substructural features which can help to identify compounds that appear as frequent hitters (promiscuous compounds) in many biochemical high throughput screens. The compounds identified by such substructural features are not recognized by filters commonly used to identify reactive compounds. Even though these substructural features were identified using only one assay detection technology, such compounds have been reported to be active from many different assays. In fact, these compounds are increasingly prevalent in the literature as potential starting points for further exploration, whereas they may not be.

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New Substructure Filters for Removal of Pan Assay Interference Compounds (PAINS) from Screening Libraries and for Their Exclusion in Bioassays

Cyclodextrin Drug Carrier Systems.

The Stability of Cyclodextrin Complexes in Solution.

Biopolymer-based hydrogels as scaffolds for tissue engineering applications: a review

Viscosities, apparent molar volumes, and activity coefficients of aqueous solutions for D-glucose, maltose, and maltotriose were measured at various concentrations. The signs of Bst, the increment of viscosity B-coefficient arising from structural change of water, were positive for these three saccharides, and the signs of dB⁄dT, the temperature dependence of B, were negative. The magnetudes of Bst and |dB⁄dT| increased with the number of glucose residue. Activity coefficients were larger than unity and increased with concentration, and their magnitudes also increased with the number of glucose residue. These results indicate that D-glucose, maltose, and maltotriose are structure forming solutes, and that their abilities lie in the order of D-glucose<maltose<maltotriose.

Studies on Aqueous Solutions of Saccharides. II. Viscosity B-Coefficients, Apparent Molar Volumes, and Activity Coefficients of D-Glucose, Maltose, and Maltotriose in Aqueous Solutions

The bioadhesive property of tablets consisting of hydroxypropyl cellulose (HPC) and carboxyvinyl polymer (CP) was investigated using the mouse peritoneal membrane. The adhesion force was significantly affected by the mixing ratio of HPC and CP in the tablet, and the weakest adhesion force was observed at the ratio of 3:2 (HPC:CP). Interpolymer complex formation was confirmed between HPC and CP in the acidic medium by turbidity and viscosity measurements. The interaction between CP carboxyl groups and HPC molecules was considered to be a possible mechanism for this complex formation on the basis of a Fourier-transform infrared spectroscopy. These observations suggested that the adhesion force of the HPC--CP tablet to the mucous membrane was significantly affected by the interpolymer complex formation between HPC and CP.

Factors affecting the bioadhesive property of tablets consisting of hydroxypropyl cellulose and carboxyvinyl polymer.

Activity coefficients of isomeric monosaccharides, D-glucose, D-mannose, and D-galactose were determined by isopiestic comparison method at 25 °C Excess partial molar entropy of water (\barSwex) of each monosaccharide solution was negative and the absolute value increased with concentration of solute From the magnitudes of negative \barSwex, it was concluded that the structure making ability among three isomers lies in the order D-glucose>D-mannose>D-galactose

Studies on Aqueous Solutions of Saccharides. I. Activity Coefficients of Monosaccharides in Aqueous Solutions at 25 °C

An anhydrous polymorphic form of trehalose

The viscosities and densities at 15, 25, and 35 °C, and activity coefficients at 25 °C for the aqueous solutions of α- and γ-cyclodextrins were measured, and the results were interpreted in terms of solute-solvent and solute-solute interactions. The concentration and temperature dependences of viscosities and apparent molar volumes are almost similar to those of linear saccharides, i.e. maltose and maltotriose, indicating that α- and γ-cyclodextrins are structure forming solutes. However, the concentration dependences of activity coefficients of cyclodextrins are significantly different from those of maltose and maltotriose. The results were tentatively assigned to the formation of dimer in aqueous solutions.

Masayuki Nakagaki

Papers

Studies on Aqueous Solutions of Saccharides. II. Viscosity B-Coefficients, Apparent Molar Volumes, and Activity Coefficients of D-Glucose, Maltose, and Maltotriose in Aqueous Solutions

Factors affecting the bioadhesive property of tablets consisting of hydroxypropyl cellulose and carboxyvinyl polymer.

Studies on Aqueous Solutions of Saccharides. I. Activity Coefficients of Monosaccharides in Aqueous Solutions at 25 °C

An anhydrous polymorphic form of trehalose

Viscosity B-coefficients, apparent molar volumes, and activity coefficients for α- and γ-cyclodextrins in aqueous solutions