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.

[Health status of the residents in the area polluted by fluorine-containing discharges from the Tajik aluminium producing plant]. / Sostoianie zdorov'ia naseleniia v raione, zagriaznennom ftorsoderzhashchimi vybrosami Tadzhikskogo aliuminievogo zavoda.

The paper presents the results of investigations and follow-up monitoring to study the environment-human health relationships in the vicinity of an aluminium plant to substantiate a complex of preventive and health-promoting measures. Experience in planning and organizing the monitoring of environmental pollution and the health status of workers and the general population may be useful in doing the same work in the vicinity of other aluminium-making works.

[Iridoangiography using indocyanine green in severely pigmented iris in clinical conditions]. / Iridoangiografiia s indotsianinom zelenym sil'nopigmentirovannoi raduzhnoi obolochki v klinike.

The authors presented the results of iridoangiography. In the course of the studies it was established that infrared light is tolerated easier than the blue one in fluorescent iridoangiography. This technique is of interest for the study of microcirculation in the vessels of the iris of the eye in inflammatory and dystrophic processes.

[Indocyanine green fluorescence iridoangiography in pigmented iris]. / Indotsianin zelenyi--fliuorestsentnaia iridoangiografiia pigmentirovannoi raduzhnoi obolochki.

Indocyanine green (ICG) fluorescent iridoangiography was used to diagnose pigmented tumors of the iris. Ten patients with pigmented tumors of the iris were examined using a modified photo-slit lamp with infrared narrow-strip optic filters. Fluorescein fluorescent iridoangiography was found ineffective. ICG fluorescent iridoangiograms have shown the vascular net and helped define the time parameters. Signs characteristic of the studied condition were defined. ICG fluorescent iridoangiography, biomicroscopy, and clinical data helped specify the diagnosis, this permitting the choice of the correct treatment strategy.

[Acute appendicitis associated with ovarian apoplexy]. / Sochetanie ostrogo appenditsita s apopleksiei iaichnikov.

Ovarian apoplexy was established in 41 (2.6%) of 1581 women operated upon with diagnosis "acute appendicitis". Apoplexy of the right ovary was found in 26 women, of the left one--in 7 women. Seven patients had bilateral ovarian apoplexy associated with acute appendicitis. In ovarian apoplexy urgent operations are indicated. In 29 women operations were started by the Volkovich-Diakonova incision, in 12 cases median laparotomy was used. Appendectomy is necessary when inflammation of the vermiform process is suspected.

[Effectiveness of certain immunologic methods in the diagnosis of acute bacterial dysentery]. / Effektivnost' nekotorykh immunologicheskikh metodov issledovaniia pri diagnostike ostroi bakterial'noi dizenterii.

The effectiveness of some immunological methods for diagnosing dysentery has been compared. This comparison has indicated that such methods as the determination of the presence of specific sensitization in the patients (by the indirect mast cell degranulation test), the detection of circulating complement-fixing antibodies to Shigella (by the complement fixation test) and antigenically reactive lymphocytes (by the lymphocyte agglutination test with the use of the antigen and by the indirect rosette-formation test) are more stable, expressive and sensitive than other serological tests and may be used for the complex clinical and laboratory diagnosis of this disease.