Modification of phenothiazine and carbazole derivatives with trifluoromethyl-containing 1,3,5-oxadiazines and imidazolidinediones

Russian Chemical Bulletin - Modification of phenothiazine and carbazole derivatives with trifluoromethyl-containing 1,3,5-oxadiazines and imidazolidinediones based on the copper(I)-catalyzed...     

Novel bicyclic derivatives of 1,3-selenazine

Bicyclic isoselenoureas (1-selena-3-azaspiro[5.5]undec-2-en-2-ylamines and 3-selena-1-azabicyclo[3.3.1]non-2-ylideneamines) were obtained by intramolecular cyclization of selenoureas leading to 1,3-selenazine ring formation and tested for antioxidant activity.     

Modification of gamma-carbolines with N-substituted propionamides as a new approach to mitoprotective agents

An approach to the modification of biologically active gamma-carbolines with the N-substituted propionamide fragments by the reaction of N-substituted acrylamides with gamma-carbolines catalyzed by cesium fluoride has been suggested. The compounds synthesized were studied for the influence on the functional characteristics of brain mitochondria, in particular, on the membrane potential, calcium-induced “swelling” and calcium capasity of the rat brain mitochondria.     

Physiologically active bis(dialkylamides) of phosphoryl-substituted α,ω-dicarboxylic acids

Bis(dialkylamides) of phosphoryl-substituted α,ω-dicarboxylic acids were synthesized and their biological activity was studied.     

Synthesis and biological activity of dialkylamino-substituted phosphine oxides

A series of dialkylamino-substituted phosphine oxides was synthesized and their physiological activity was studied.     

Local ergodicity for systems with growth properties including multi-dimensional dispersing billiards

We prove local ergodicity of uniformly hyperbolic discrete time dynamical systems with singularities, which satisfy certain regularity conditions and an assumption on the growth of unstable manifolds. We apply the result to prove ergodicity of a class of multi-dimensional dispersing billiards.     

Host–guest complexation in the β-glycyrrhizic acid–2,8-dimethyl-5-[2´-(6″-methylpyridin-3″-yl)ethyl]-2,3,4,5-tetrahydro-1<Emphasis Type="Italic">H</Emphasis>-pyrido[4,3-<Emphasis Type="Italic">b</Emphasis>]indole system

Electronic, IR, and NMR spectroscopy methods were used to study the interaction in the β-glycyrrhizic acid (GA)–2,8-dimethyl-5-[2´-(6″-methylpyridin-3″-yl)ethyl]-2,3,4,5-tetra-hydro-1H-pyrido[4,3-b]indole (Dim) system in an alcoholic medium. The complete assignment of signals in the ¹H and ¹³C NMR spectra of Dim and GA in CD₃OD was made for the individual components and for thier mixtures at different ratios. These data suggest the formation of a host–guest complex in this system. It is hypothesized that associates of GA molecules interact with Dim through Δ^12,13–carbonyl group conjugated bonds in the triterpene moiety of GA that interact with the aromatic systems of the indole and pyridine moieties of Dim, as well as via an acid-base mechanism involving mainly the carboxy groups of glucuronic acid residues in the carbohydrate part of GA and the nitrogen atom of the tetrahydropyridine ring of Dim.     

Targeted synthesis and biological activity of polypharmacophoric agents for the treatment of neurodegenerative diseases

Synthetic approaches to the design of new multitarget agents for the treatment of neurodegenerative diseases are surveyed. These approaches are based on the conjugation of the pharmacophoric indole, phenothiazine, and aminoadamantane moieties via 1-oxopropylene and 2-hydroxypropylene spacers using reactions of acrylate- and epoxide-containing pharmacophores with tetrahydro-γ-carbolines, cycloalkaneindoles, carbazoles, and aminoadamantanes. The review considers data on biological activity of the compounds assessed within a complex screening system. This system includes neurotransmitter targets associated with cognitive compensation, such as cholinesterases and glutamate receptors, mitochondria, the influence on which can provide neuroprotective effects, and microtubules, the stabilization of which leads to the improvement of axonal transport. The ability of the compounds to act as free-radical scavengers was evaluated. Types of polypharmacophoric compounds promising for further development are proposed.