Thiacalixarene based quaternary ammonium salts as promising antibacterial agents.

The search for new antibacterial and antiseptic drugs is an urgent problem due to the resistance of microorganisms to existing drugs. In this work, for the first time, the design of antibacterial and bactericidal agents based on quaternary ammonium compounds on thiacalixarene macrocyclic platform was proposed and implemented. A series of tetrasubstituted quaternary ammonium salts with different nature and length of the substituent (-N+(CH3)2R, R = CH2Ph, CnH2n+1, n = 1, 4, 8, 10) based on p-tert-butylthiacalix[4]arene in cone and 1,3-alternate conformations was obtained with excellent yields. The obtained compounds have a high antibacterial effect against Gram-positive (S. aureus, S. epidermidis, B. subtilis) bacteria comparable with commercial antiseptics chlorhexidine, miramistin and benzalkonium chloride. It was found that quaternary ammonium derivatives of thiacalix[4]arene in 1,3-alternate conformation more effectively inhibit the growth of the tested bacterial strains in comparison with compounds in cone conformation. Cytotoxicity studies on human skin fibroblast (HSF) cells demonstrated that all compounds were less toxic compared to reference drugs. The different type of interaction of the studied compounds with model DPPC lipid membranes explains different antibacterial activity and cytotoxicity of compounds. The compounds in cone conformation are adsorbed on the DPPC vesicles membrane surface, while the incorporation of lipophilic alkyl fragments of macrocycles in 1,3-alternate conformation into the membrane leads to "clumping" of DPPC vesicles. It was shown the saving of antibacterial activity of thiacalixarene derivatives in 1,3-alternate conformation on Gram-positive clinical strains. The obtained results allow viewing the described thiacalixarene based quaternary ammonium compounds as promising molecules in the development of the new antibacterial agents.

Comment on "An unexpected formation of the novel 7-oxa-2-azabicyclo[2.2.1]hept-5-ene skeleton during the reaction of furfurylamine with maleimides and their bioprospection using a zebrafish embryo model" by C. E. Puerto Galvis and V. V. Kouznetsov, Org. Biomol. Chem., 2013, 11, 407.

It has been proved that the reaction between furfuryl amines and N-R-maleimides leads to the formation of aza-Michael addition products - 3-(furylmethylamino)-N-R-pyrrolidine-2,5-diones, instead of 7-oxa-2-azabicyclo[2.2.1]hept-5-enes, as this journal reported previously.

Diffusive Propagation of Exciton-Polaritons through Thin Crystal Slabs.

If light beam propagates through matter containing point impurity centers, the amount of energy absorbed by the media is expected to be either independent of the impurity concentration N or proportional to N, corresponding to the intrinsic absorption or impurity absorption, respectively. Comparative studies of the resonant transmission of light in the vicinity of exciton resonances measured for 15 few-micron GaAs crystal slabs with different values of N, reveal a surprising tendency. While N spans almost five decimal orders of magnitude, the normalized spectrally-integrated absorption of light scales with the impurity concentration as N(1/6). We show analytically that this dependence is a signature of the diffusive mechanism of propagation of exciton-polaritons in a semiconductor.

Super-radiant mode in InAs-monolayer-based Bragg structures.

We report direct experimental evidence of the collective super-radiant mode in Bragg structure containing 60 InAs monolayer-based quantum wells (QWs) periodically arranged in GaAs matrix. Time-resolved photoluminescence measurements reveal an appearance of the additional super-radiant mode, originated from coherent collective interaction of QWs. This mode demonstrates a super-linear dependence of the intensity and radiative decay rate on the excitation power. The super-radiant mode is not manifested in the case if only a small number of QWs is excited.

Physiological mechanisms of the "arousal response" in animals in a state of hypobiosis.

In a state of hypobiosis in white rats it was found that the previously described [4, 6] "arousal response" is characterized by a flareup of motor activity with a definite coordinated structure of the motor acts in response to a change in the animal's posture. Repeated reproduction of this response leads to a rapid summation of the electromyographic activity and a rise in the temperature. In experiments on heterothermic animals these responses are even more pronounced and are accompanied by a restoration of the original body posture and substantial temperature rise. Such an effective process of heat formation in the bodies of heterothermic animals during the "arousal response" may be associated with the mechanism of "special" awakening under conditions of reduced activity.

[Basic approaches to medical, forensic, and biomechanical studies in expert evaluation of a car injury]. / Printsipy podkhoda k mediko-trassologicheskim i biokhimicheskim issledovaniiam pri ékspertize avtomobil'noi travmy.

Modern approaches to forensic medical expert evaluation of car injuries are discussed. Many problems remain unsolved after examination of injuries in victims inside the car, which negatively tells on the versions suggested during criminal investigation of car accidents. The experts often neglect the most sensitive methods for evaluation of these injuries and many fundamental approaches to the problem: differential diagnosis of primary and secondary injuries; basic medical and biomechanical methods and studies of the clues; fundamentals of total systems evaluation of the results of forensic medical expert evaluation.

[Alternative pathways of the initial transformation of 2,4,6-trinitrotoluene by yeasts]. / Al'ternativnye puti nachal'noi transformatsii 2,4,6-trinitrotoluola drozhzhami.

A new model for the initial transformation of 2,4,6-trinitrotoluene (TNT) by facultatively anaerobic and aerobic yeasts is presented. The model is based on the data that Saccharomyces sp. ZS-A1 was able to reduce the nitrogroups of TNT with the formation of 2- and 4-hydroxyaminodinitrotoluenes (2-HADNT and 4-HADNT) as the major early TNT metabolites (the molar HADNT/TNT ratio reached 0.81), whereas aminodinitrotoluenes (ADNTs) and the hydride-Meisenheimer complex of TNT (H-TNT) were the minor products. Candida sp. AN-L13 almost completely transformed TNT into H-TNT through the reduction of the aromatic ring. Candida sp. AN-L14 transformed TNT through a combination of the two mechanisms described. Aeration stimulated the production of HADNT from TNT, whereas yeast incubation under stationary conditions promoted the formation of HADNT. The transformation of TNT into HADNT led to a tenfold increase in the acute toxicity of the TNT preparation with respect to Paramecium caudatum, whereas the increase in the toxicity was about twofold in the case of the alternative attack at the aromatic ring.

[Distribution and physiology of microorganisms in petrochemical oily sludge of plant]. / Osobennosti raspredeleniia i fiziologicheskogo sostoianiia mikroorganizmov nefteshlama--otkhoda neftekhimicheskogo proizvodstva.

The occurrence, vertical distribution, and the physiological state of microorganisms in a petrochemical oily sludge deposit were studied. The total number and the number of viable microbial cells at depths of 0.2 and 3 m were about 10 and 10(8) cells/g dry wt. sludge. Most microbial cells taken from the middle (1 m deep) and the bottom (3 m deep) sludge horizons showed a delayed colony-forming ability, which suggested that the cells occurred in a hypometabolic state. The relative number of microaerobic denitrifying microorganisms steeply increased with depth. The amount of microorganisms tolerant to 3, 5, and 10% NaCl and capable of growing at 7 and 40 degrees C varied from 10(2) to 10(8) CFU/g dry wt. sludge. Petrochemical oily sludge was found to maintain the growth of heterotrophs, among which the degraders of oily sludge and ten different individual polycyclic aromatic hydrocarbons were detected. The occurrence of highly adaptable microorganisms with an adequate metabolic potential in the petrochemical oily sludge deposit implies that its bioremediation is possible without introducing special microorganisms.