Reaction Products of β-Aminopropioamidoximes Nitrobenzenesulfochlorination: Linear and Rearranged to Spiropyrazolinium Salts with Antidiabetic Activity.

Nitrobenzenesulfochlorination of β-aminopropioamidoximes leads to a set of products depending on the structure of the initial interacting substances and reaction conditions. Amidoximes, functionalized at the terminal C atom with six-membered -heterocycles (piperidine, morpholine, thiomorpholine and phenylpiperazine), as a result of the spontaneous intramolecular heterocyclization of the intermediate reaction product of an S2 substitution of a hydrogen atom in the oxime group of the amidoxime fragment by a nitrobenzenesulfonyl group, produce spiropyrazolinium or -nitrobenzenesulfonates. An exception is -nitrobenzenesulfochlorination of β-(thiomorpholin-1-yl)propioamidoxime, which is regioselective at room temperature, producing two spiropyrazolinium salts (-nitrobezenesulfonate and chloride), and regiospecific at the boiling point of the solvent, when only chloride is formed.

Synthesis and biological evaluation of new derivatives of grossheimin.

Grossheimin 1 is a polyfunctionalized sesquiterpene, featuring, in addition to the exomethylene-γ-lactone group, also an additional exocyclic double bond, a hydroxyl, and a ketone carbonyl. These functional groups have been modified, generally in an orthogonal way, by arylation of the exomethylene, by the introduction of heteroatoms associated to oxygen-, nitrogen- and phosphorous functionalities, and by acylation. A selection of the analogues was investigated for bioactivity, showing that the introduction of a substituent at C-13 is not detrimental, and can modulate potency independently from retention or reduction of the C-11 - C-13 exomethylene double bond and the effect of this maneuver on Michael reactivity.

Anatomical study and histochemical analysis of Artemisia leucodes Schrenk.

The study of anatomical structure of the aerial part of Artemisia leucodes Schrenk. was carried out, and in this regard, the anatomical and diagnostic features of A. leucodes raw materials were revealed: epidermal cells of an elongated shape, mesophyll in the leaves is columnar, the stem has a fascicular structure, collenchymal mechanical structures are present in the stem ribs.

Inhibition of T Cell Receptor Activation by Semi-Synthetic Sesquiterpene Lactone Derivatives and Molecular Modeling of Their Interaction with Glutathione and Tyrosine Kinase ZAP-70.

A variety of natural compounds have been shown to modulate T cell receptor (TCR) activation, including natural sesquiterpene lactones (SLs). In the present studies, we evaluated the biological activity of 11 novel semi-synthetic SLs to determine their ability to modulate TCR activation. Of these compounds, α -epoxyarglabin, cytisinyl epoxyarglabin, 1 β ,10 α -epoxyargolide, and chloroacetate grosheimin inhibited anti-CD3-induced Ca mobilization and extracellular signal-regulated kinase 1/2 (ERK1/2) phosphorylation in Jurkat T cells.