Potent and highly selective dual-targeting monoamine oxidase-B inhibitors: Fluorinated chalcones of morpholine versus imidazole.

Two series of fluorinated chalcones containing morpholine and imidazole-based compounds (f1-f8) were synthesized and evaluated for recombinant human monoamine oxidase (MAO)-A and -B as well as acetylcholinesterase inhibitory activities. Our results indicate that morpholine containing chalcones are highly selective MAO-B inhibitors having reversibility properties. All the imidazole-based fluorinated chalcones showed weak MAO inhibitions in both isoforms. Among the tested compounds, (2E)-3-(3-fluorophenyl)-1-[4-(morpholin-4-yl)phenyl]prop-2-en-1-one (f2) showed potent inhibitory activity for recombinant human MAO-B (IC50 = 0.087 µM) with a high selectivity index (SI) of 517.2. In the recovery experiments using dialysis, the residual activity of MAO-B inhibited by f2 was close to that with the reversible reference inhibitor. Inhibition assays revealed that the Ki values of f1 and f2 for MAO-B were 0.027 and 0.020 µM, respectively, with competitive patterns. All the morpholine-based compounds (f1-f4) showed moderate inhibition toward acetylcholinesterase with IC50 values ranging between 24 and 54 µM. All morpholine-containing compounds exhibit good blood-brain barrier permeation in the PAMPA method. The rational approach regarding the highly selective MAO-B inhibitor f2 was further ascertained by induced fit docking and molecular dynamics simulation studies.

A new patterning method using photocatalytic lithography and selective atomic layer deposition.

We report a new patterning method using photocatalytic lithography of alkylsiloxane self-assembled monolayers and selective atomic layer deposition of thin films. The photocatalytic lithography is based on the fact that the decomposition rate of the alkylsiloxane monolayers in contact with TiO2 is much faster than that with SiO2 under UV irradiation in air. The photocatalytic lithography, using a quartz plate coated with patterned TiO2 thin films, was done to prepare patterned monolayers of the alkylsiloxane on Si substrates. A ZrO2 thin film was selectively deposited onto the monolayer-patterned Si substrate by atomic layer deposition.