Subthalamic nucleus gamma activity increases not only during movement but also during movement inhibition.

Gamma activity in the subthalamic nucleus (STN) is widely viewed as a pro-kinetic rhythm. Here we test the hypothesis that rather than being specifically linked to movement execution, gamma activity reflects dynamic processing in this nucleus. We investigated the role of gamma during fast stopping and recorded scalp electroencephalogram and local field potentials from deep brain stimulation electrodes in 9 Parkinson's disease patients. Patients interrupted finger tapping (paced by a metronome) in response to a stop-signal sound, which was timed such that successful stopping would occur only in ~50% of all trials. STN gamma (60-90 Hz) increased most strongly when the tap was successfully stopped, whereas phase-based connectivity between the contralateral STN and motor cortex decreased. Beta or theta power seemed less directly related to stopping. In summary, STN gamma activity may support flexible motor control as it did not only increase during movement execution but also during rapid action-stopping

1-Isocyanomethylbenzotriazole and 2,2,4,4-tetramethylbutylisocyanide-cleavable isocyanides useful for the preparation of α-aminomethyl tetrazoles

1-Isocyanomethylbenzotriazole and 2,2,4,4-tetramethylbutylisocyanide smoothly undergo Ugi type reaction toward 1,5-disubstituted aminomethyl tetrazoles and can be subsequently cleaved under acidic conditions yielding substituted α-aminomethyl tetrazoles. © 2006 Elsevier Ltd. All rights reserved

A novel three-component butenolide synthesis.

[reaction: see text]. 5-Acylamino butenolides can be assembled by a multicomponent reaction (MCR) of isocyanides, glyoxals, and acetophosphonic acid diethylesters, followed by a intramolecular Wittig-type reaction. The reaction can be performed either in one pot or with the isolation of the intermediate Passerini product. This versatile reaction offers three independent inputs displayed in the final product. Applications in combinatorial chemistry and natural product synthesis can be envisioned

Short and diverse route toward complex natural product-like macrocycles.

[reaction: see text] A general strategy toward macrocyclic compounds using multicomponent reaction (MCR) chemistry, e.g., Passerini and Ugi variants, and ring-closing metathesis (RCM) is introduced. The corresponding bifunctional isocyanides carboxylic acids bearing a terminal olefin are easy to prepare from the corresponding commercially available starting materials. Advantageously, this strategy allows fast access to a diverse conformational space of natural product-like macrocycles and could thus be of interest in the discovery of novel bioactive agents

CCDC 200226: Experimental Crystal Structure Determination

Related Article: Eman M.M. Abdelraheem, Shabnam Shaabani, Alexander Dömling|2018|Drug Discovery Today:Technol.|29|11|doi:10.1016/j.ddtec.2018.06.008,Related Article: B.Beck, G.Larbig, B.Mejat, M.Magnin-Lachaux, A.Picard, E.Herdtweck, A.Domling|2003|Org.Lett.|5|1047|doi:10.1021/ol034077e,An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.