A series of thiomorpholine sulfonamide hydroxamate TACE inhibitors, all bearing propargylic ether P1' groups, was explored. In particular, compound 5h has excellent in vitro potency against isolated TACE enzyme and in cells, oral activity in a model of TNF-alpha production
Chemistry (Weinheim an der Bergstrasse, Germany), 14(2), 747-753 (2007-10-24)
We demonstrate the supramolecular and structural equivalence of two halogen-bond donors (I and Br) and three acceptors (O, NH and S) through the synthesis of seven isostructural halogen-bonded cocrystals, involving six different molecules: 1,4-dibromo- and 1,4-diiodotetrafluorobenzene (donors) and thiomorpholine, thioxane
Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy, 58(12), 2737-2757 (2002-10-25)
The natural abundance 15N-NMR chemical shifts of selected aliphatic amines, 2-substituted pyridine type compounds, bialicyclic tertiary amines have been measured as a function of the nature of the solvent. In the case of cyclic aliphatic amines, like piperidine, morpholine, piperazine
A screening of lignin-degrading basidial fungi that can grow in the presence of thiomorpholine derivatives (the mixture of 1,4-perhydrothiazines) has been performed. Strain Bjerkandera adusta VKM F-3477 was shown to have the maximal rate of growth in the presence of
We designed two novel thiolactone scaffolds. Both scaffolds can be accessed by a convergent Ugi multicomponent reaction (MCR) and are, thus, amenable to library synthesis. Design, stereoselectivity, structures, full experimental details, and virtual libraries will be reported.
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