Prospects for application of microorganisms in bioremediation of soils contaminated with pesticides.

The contamination of soil with residual amounts of pesticides remains an urgent challenge for human community. The most efficient approach to address this challenge is the direct microbial degradation of a pesticide in agricultural lands. To this end, the selected microorganisms, which quickly and completely utilize pesticides, are employed. In the present work, two herbicides belonging to different classes of chemical compounds, that is, imazamox and chlorsulfuron were used. The screening of promising microorganisms was carried out among different strains of bacteria and fungi in a liquid mineral medium containing a pesticide as the only source of carbon. It was found that the most active microorganisms were capable of utilizing up to 90% of the active substance for a short time. The dynamics of pesticides degradation indicated that the maximum destruction of the studied substances occurred during the first two weeks of cultivation. Further, the rate of degradation dramatically dropped or stopped at all. An increase in the concentration of pesticides in the cultivation medium almost completely suppressed their degradation. It is interesting that the bacteria were more suitable for the degradation of imazamox, while the fungi rendered the destruction of chlorsulfuron.

Design of novel water-soluble isoxazole-based antimicrobial agents and evaluation of their cytotoxicity and acute toxicity.

Based on the readily available 3-organyl-5-(chloromethyl)isoxazoles, a number of previously unknown water-soluble conjugates of isoxazoles with thiourea, amino acids, some secondary and tertiary amines, and thioglycolic acid were synthesized. The bacteriostatic activity of aforementioned compounds has been studied against Enterococcus durans B-603, Bacillus subtilis B-407, Rhodococcus qingshengii Ac-2784D, and Escherichia coli B-1238 microorganisms (provided by All-Russian Collection of Microorganisms, VKM). The influence of the nature of the substituents in positions 3 and 5 of the isoxazole ring on the antimicrobial activity of the obtained compounds has been determined. It is found that the highest bacteriostatic effect is observed for compounds containing 4-methoxyphenyl or 5-nitrofuran-2-yl substituents in position 3 of the isoxazole ring as well as methylene group in position 5 bearing residues of l-proline or N-Ac-l-cysteine (5a-d, MIC 0.06-2.5 µg/ml). The leading compounds showed low cytotoxicity on normal human skin fibroblast cells (NAF1nor) and low acute toxicity on mice in comparison with the well-known isoxazole-containing antibiotic oxacillin.

A Novel Family of [1,4]Thiazino[2,3,4-ij]quinolin-4-ium Derivatives: Regioselective Synthesis Based on Unsaturated Heteroatom and Heterocyclic Compounds and Antibacterial Activity.

A novel family of [1,4]thiazino[2,3,4-ij]quinolin-4-ium derivatives was synthesized by annulation reactions of 8-quinolinesulfenyl chloride with unsaturated heteroatom and heterocyclic compounds. It was found that the reactions with 4-pentenoic and 5-hexenoic acids, allyl chloride and bromide, allyl cyanate and vinyl heterocyclic compounds (N-vinyl pyrrolidin-2-one and 1-vinylimidazole) proceeded in a regioselective mode but with the opposite regiochemistry. The reactions with vinyl heterocyclic compounds included electrophilic addition of the sulfur atom of 8-quinolinesulfenyl chloride to the ß-carbon atom of the vinyl group. In the case of other substrates, the annulation proceeded with the attachment of the sulfur atom to the α-carbon atom of the vinyl group. The antibacterial activity of novel water-soluble compounds against Enterococcus durans, Bacillus subtilis and Escherichia coli was evaluated. Compounds with high antibacterial activity were found.

Complete Genome Sequence of Rhodococcus qingshengii Strain VKM Ac-2784D, Isolated from Elytrigia repens Rhizosphere.

Rhizosphere bacteria are considered to be promising destructors of oil and its components. Bacterial species of the genus Rhodococcus can degrade a variety of hydrocarbons and are widely used for the bioremediation of polluted environments. Here, we report the complete genome sequence of Rhodococcus qingshengii strain VKM Ac-2784D.

Arabinogalactan propargyl ethers: Au-catalysed hydroamination by imidazols.

A method for the synthesis of pharmacologically prospective arabinogalactan (AG) imidazole- and benzimidazole derivatives in a yield of up to 97 % via Au(III)-catalyzed hydroamination of AG propargyl ethers has been developed. It is found that in the presence of 5 mol% HAuC14 and 10-fold excess imidazole relative to the propargyl groups, the hydroamination successfully competes with cross-linking processes to afford products soluble in DMSO and aqueous HC1 solutions (degree of substitution of imidazolylpropenyl fragments 0.5-1.8, yield 62-97 %). It is established that under the conditions of hydroamination Au(III) is reduced to give mainly Au(0) and minor amounts of Au(I), which are contained in AG imidazole derivatives as particles of 190-640 nm in size. Hydrochlorides of Au-containing AG imidazole derivatives show high bacteriostatic activity with respect to test gram-positive microorganisms and thus confirming their prospects as new AG-derived bioactive agents.