Reversible Small Molecule Inhibitors of MAO A and MAO B with Anilide Motifs.

Background: Ligands consisting of two aryl moieties connected via a short spacer were shown to be potent inhibitors of monoamine oxidases (MAO) A and B, which are known as suitable targets in treatment of neurological diseases. Based on this general blueprint, we synthesized a series of 66 small aromatic amide derivatives as novel MAO A/B inhibitors.

Methods: The compounds were synthesized, purified and structurally confirmed by spectroscopic methods.

SAR of Sponge-Inspired Hemibastadin Congeners Inhibiting Blue Mussel PhenolOxidase.

Hemibastadin derivatives, including the synthetically-derived 5,5'-dibromohemibastadin-1 (DBHB), are potent inhibitors of blue mussel phenoloxidase (PO), which is a key enzyme involved in the firm attachment of this invertebrate to substrates and, thus, a promising molecular target for anti-fouling research. For a systematic investigation of the enzyme inhibitory activity of hemibastadin derivatives, we have synthesized nine new congeners, which feature structural variations of the DBHB core structure. These structural modifications include, e.

Histamine H₄ Receptor Antagonists: A New Approach for Tinnitus Treatment?

Tinnitus, a disorder with disruptive sound perception in the head without an external source, affects around 15 % of the worldwide adult population. Since there is no approved drug for the treatment for this symptom, novel strategies need to be developed to provide relief for the patient. A patent from the small French start-up company Sensorion suggests the use of histamine H4 receptor (H4R) inhibitors as potential treatment.

[Selection and estimation of meals by children of different ages].

With regard to the reported knowledge concerning the health value of food in 9-10-year-old children (DGE, 1984) the question arose of whether this knowledge is also valid if pupils have to evaluate meals. Twenty-seven photos of meals (9 each of breakfast, lunch and supper) were presented to 252 children of the age groups 6-7, 9-10 and 12-13 years. By means of these photos, they were requested to organize their meals for 3 days.