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
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.
Spectrophotometric assays of Mycobacterium aurum MO1 cells extracts gave evidence of a soluble cytochrome P450, involved in the degradative pathway of morpholine, a waste product from the chemical industry. In order to get further information, the kinetics of the biodegradation
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
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