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Michael addition of thiourea to enones with subsequent intramolecular aminal ether formation provided easy access to furo[2,3-d]thiazinamines and pyrano[2,3-d][1,3]thiazin-2-amines. These amines served as versatile intermediates to a variety of beta-amyloid cleaving enzyme-1 (BACE1) inhibitors. [ABSTRACT FROM AUTHOR]

Mesoporous spheres of calcium silicatehydrate (MS-CSH) have beenprepared by an ultrasonic method. Following an earlier work in whichwe have revealed the interactions between ibuprofen (IBU) and CSHcarriers with different morphologies by X-ray absorption near edgestructures (XANES) analysis. In the present investigation, two newdrug molecules, alendronate sodium (ALN) and gentamicin sulfate (GS),were incorporated into MS-CSH, and their drug loading capacities (DLCs)were measured using thermogravimetric analysis to establish the relationshipbetween drug-carrier interactions and DLCs. The XANES spectra clearlyindicate that acidic functional groups of the drug molecules linkedto the active sites (Ca–OH and Si–OH groups) of MS-CSHon the surface by electrostatic interactions. In addition, it is foundthat the stoichiometric ratio of Ca2誉 of CSH carriersand the functional groups of drug molecules may significantly influencethe DLCs. [ABSTRACT FROM AUTHOR]