60211-57-6Relevant articles and documents
Preparation of novel analogs of 2-arylpiperidines and evaluation of their sigma receptor binding affinities
Martin, Stephen F.,Walby, Grant D.
supporting information, (2022/04/09)
A number of substituted norbenzomorphans have been previously identified as high affinity ligands for the two known sigma receptors σ1R and σ2R/TMEM97, and some norbenzomorphans that are selective for σ2R/TMEM97 exhibit promise in animal models of several neurological disorders. Toward further assessing the effects of simplifying the norbenzomorphan scaffold, sets of 6-membered heterocycles were designed and prepared, and their binding affinities for σ1R and σ2R/TMEM97 were determined. Consistent with our design strategy, N-acyl-2-arylpiperidines show high affinity for σ2R/TMEM97, whereas those derived from morpholine and N-methylpiperazine have lower affinities. However, most of these 6-membered heterocycles unexpectedly exhibit even higher affinity for σ1R and are thus σ1R-selective. Computational docking studies show that representative 6-membered heterocycles bind and interact with σ2R/TMEM97 in a manner similar to that of a docked structure of their norbenzomorphan parent. Collectively, these binding and computational studies support our design strategy for developing simplified analogs of norbenzomorphans as σ2R/TMEM97 ligands, but they also underscore the challenges associated with developing selective modulators of σ2R/TMEM97.
Silica-coated Fe3O4 magnetic nanoparticles-supported sulfonic acid as a highly active and reusable catalyst in chemoselective deprotection of tert-butyldimethylsilyl (TBDMS) ethers
Hossein Javadi, Sayed,Zareyee, Daryoush,Monfared, Azam,Didehban, Khadijeh,Mirshokraee, Sayed Ahmmad
supporting information, p. 7 - 12 (2019/11/03)
Anchored propyl sulfonic acid on the surface of silica-coated magnetic nanoparticles (Fe3O4@SiO2@PrSO3H) was successfully employed in the deprotection of TBDMS ethers. The prepared magnetically separable nanocatalyst exhibited efficient catalytic activity with high conversion and selectivity in cleavage of TBDMS ethers. TBDMS ethers are efficiently cleaved to the corresponding hydroxyl compounds in methanol solution containing 2 mol% magnetic nano-catalysts. Good to excellent yields of products, simple work-up and product separation, selective cleavage of TBDMS ethers in the presence of TBDPS ethers, easy recycling of the catalyst with external magnet with no loss in its activity (7 reaction cycles) are important features of this new protocol.
AMINO ACID DERIVATIVES AND THEIR USE AS THROMBIN INHIBITORS
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, (2008/06/13)
There is provided compounds of formula I, wherein R 1, R 2, R 3, R x, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required as in thrombosis or as anticoagulants.
