Synthesis and properties of low-molecular-weight copolymers of acrylamide with 2-acrylamido-2-methylpropanesulfonic acid,as potential drug carriers

Nontoxic water-soluble low-molecular-weight (MW 14 000–36 000 Da) copolymers of acrylamide with 2-acrylamido-2-methylpropanesulfonic acid, containing from 17.3 to 37.6 mol % sulfonate-containing monomeric units, were synthesized by heterophase radical polymerization in isopropanol or ethanol at 50°C with azobis(isobutyronitrile) as an initiator. Original Russian Text M.V. Solovskii, M.Yu. Eropkin, E.M. Eropkina, A.V. Slita, M.Yu. Smirnova, E.N. Vlasova, E.B. Tarabukina, A.I. Amirova, 2007, published in Zhurnal Prikladnoi Khimii, 2007, Vol. 80, No. 10, pp. 1674–1678.     

Highly efficient and stereoselective cycloaddition of nitrones to indolyl- and pyrrolylacrylates

The reactions of various nitrones with indolyl- and pyrrolylacrylates proceeds regioselectively with high diastereoselectivity in the case of aldonitrones, and represents an effective method for obtaining new indolyl- and pyrrolyl-substituted isoxazolidine carboxylates stabilized by weak (CH?O) and moderate (NH?N) strength intramolecular hydrogen bonding. The resulting cycloadducts exhibit promising in vitro anti-influenza activities.     

Alkylated chitosans of low molecular weight as non-viral transfection vectors for gene therapy

Low molecular weight chitosans (5 kDa) hydrophobically modified with 3, 10, and 18 mol % of tetradecenoyl (TDC) groups have been synthesized. Their good solubility at neutral pH, their surface activity and micelle-forming properties as well as their ability to interact with negatively charged phospholipid vesicles mimicking the internal layer of cell plasma membranes, allow us to consider them as potential non-viral transfection vectors for gene therapy.     

Synthesis and antiviral activity of novel 3-substituted pyrazolinium salts

Chemistry of Heterocyclic Compounds - For the first time, convenient methods for the preparation of pyrazoline N-alkylidene salts based on terpene (camphor, camphorquinone, carvone) ketones, cage...     

The 1,3-dipolar cycloaddition of adamantine-derived nitrones with maleimides

Abstract

Adamantane-derived aldo- and ketonitrones react with maleimides giving corresponding isoxazolidines. In the case of aldonitrones reactions proceed giving the diastereomeric mixtures. The ratio of isomers is changing during the reaction process due to the reversibility of the cycloaddition reaction. The cytotoxic and virus-inhibiting activity against influenza virus was investigated for selected adducts.     

Synthesis of 1,2,3-triazolyl nucleoside analogues and their antiviral activity

Molecular Diversity - Based on the fact that a search for influenza antivirals among nucleoside analogues has drawn very little attention of chemists, the present study reports the synthesis of a...     

Search for Compounds with Antiviral Activity Among Maleopimaric Acid Derivatives

Chemistry of Natural Compounds - Three new maleopimaric acid derivatives were synthesized. The antiviral activity of 14 synthesized maleopimaric acid derivatives was tested against influenza virus...     

Control of chaotic oscillations of a satellite

Analytical conditions and practical methods of their realization are proposed to solve a problem of a command signal tracking for a nonlinear disturbed system.Non- linear disturbed plants consisting of linear dynamic block and nonlinear block in feedback are considered.Nonlinear part of the plant and disturbance are unknown and bounded. The paper illustrates a possibility of applications of proposed algorithms to control libra- tion angle of satellite.     

Water-Soluble Polymeric Methanofullerene and Fulleropyrrolidine Derivatives

Water-soluble methanofullerene and fulleropyrrolidine derivatives were synthesized by the reactions of methanofullerenes (MFs) and fulleropyrrolidines (FPs) with poly(N-vinylpyrrolidone) (PVP) bearing one terminal amino group. The products contain MF or FP covalently bound to the polymer, corresponding polymeric complexes, and unreacted PVP. Large aggregates of the polymeric MF and FP derivatives are found in aqueous solutions. The electrooptical properties of the products differ considerably from those of the initial polymer. The phosphorus-containing MF and FP derivatives are capable of cleaving the molecule of plasmid DNA.     

Synthesis and Antiviral Evaluation of Nucleoside Analogues Bearing One Pyrimidine Moiety and Two D-Ribofuranosyl Residues

A series of 1,2,3-triazolyl nucleoside analogues in which 1,2,3-triazol-4-yl-β-d-ribofuranosyl fragments are attached via polymethylene linkers to both nitrogen atoms of the heterocycle moiety (uracil, 6-methyluracil, thymine, quinazoline-2,4-dione, alloxazine) or to the C-5 and N-3 atoms of the 6-methyluracil moiety was synthesized. All compounds synthesized were evaluated for antiviral activity against influenza virus A/PR/8/34/(H1N1) and coxsackievirus B3. Antiviral assays revealed three compounds, 2i, 5i, 11c, which showed moderate activity against influenza virus A H1N1 with IC₅₀ values of 57.5 µM, 24.3 µM, and 29.2 µM, respectively. In the first two nucleoside analogues, 1,2,3-triazol-4-yl-β-d-ribofuranosyl fragments are attached via butylene linkers to N-1 and N-3 atoms of the heterocycle moiety (6-methyluracil and alloxazine, respectively). In nucleoside analogue 11c, two 1,2,3-triazol-4-yl-2′,3′,5′-tri-O-acetyl-β-d-ribofuranose fragments are attached via propylene linkers to the C-5 and N-3 atoms of the 6-methyluracil moiety. Almost all synthesized 1,2,3-triazolyl nucleoside analogues showed no antiviral activity against the coxsackie B3 virus. Two exceptions are 1,2,3-triazolyl nucleoside analogs 2f and 5f, in which 1,2,3-triazol-4-yl-2′,3′,5′-tri-O-acetyl-β-d-ribofuranose fragments are attached to the C-5 and N-3 atoms of the heterocycle moiety (6-methyluracil and alloxazine respectively). These compounds exhibited high antiviral potency against the coxsackie B3 virus with IC₅₀ values of 12.4 and 11.3 µM, respectively, although both were inactive against influenza virus A H1N1. According to theoretical calculations, the antiviral activity of the 1,2,3-triazolyl nucleoside analogues 2i, 5i, and 11c against the H1N1 (A/PR/8/34) influenza virus can be explained by their influence on the functioning of the polymerase acidic protein (PA) of RNA-dependent RNA polymerase (RdRp). As to the antiviral activity of nucleoside analogs 2f and 5f against coxsackievirus B3, it can be explained by their interaction with the coat proteins VP1 and VP2.