Bicyclic Piperazine Mimetics of the Peptide β-Turn Assembled via the Castagnoli-Cushman Reaction.

5-Oxopiperazine-2-carboxamides and respective carboxylic acids (obtained by the Castagnoli-Cushman reaction of protected iminodiacetic anhydride) were converted into cis- and trans-configured bicyclic piperazines containing two stereogenic centers. The latter are not only well-established mimetics of peptide β-turn but also attractive, high-F cores for drug design in general. The methodology was applied to the preparation of ring-expanded version of bicyclic piperazines not described in the literature.

Microspherical Particles of Solid Dispersion of Polyvinylpyrrolidone K29-32 for Inhalation Administration.

Inhalation administration is a promising alternative to the invasive drug delivery methods. The particle size required for ideal drug aerosol preparation is between 1 and 3 m. The application of microspherical particles of solid dispersions enhances bioavailability of poorly soluble drugs due to the solubilization.

A study of the formation of magnetically active solid dispersions of phenacetin using atomic and magnetic force microscopy.

A lot of pharmaceutical substances have a poor solubility that limits their absorption and distribution to the targeted sites to elicit the desired action without causing untoward effects on healthy cells or tissues. For such drugs, new modes of delivery have to be developed for efficient and effective delivery of the drug to the target site. Formation of magnetically active solid dispersion of such drugs could be a useful approach to addressing this problem because they combine targeted delivery and good solubility.

Thermodynamics of dissolution and infrared-spectroscopy of solid dispersions of phenacetin.

In this work enthalpies of dissolution in water of polyethylene glycols (PEGs) having an average molecular weight of 1000 and 1400, Pluronic-F127, phenacetin as well as the composites prepared from them were measured using solution calorimetry at 298.15 K. Intermolecular interaction energies of polymer-phenacetin were calculated on the basis of an additive scheme.

[The effect of the acetylation phenotype on the course severity and outcome of acute viral hepatitis B].

Acetylation phenotype was studied in 70 inpatients with acute viral hepatitis B. Of them, 51 had fast and 19 slow acetylation. Fast-type acetylation was associated with mild-severe form of hepatitis B, while slow-type acetylation--with recurrences and aggravations, severe form of hepatitis.

[Regulation of terephthalate catabolism in Rhodococcus rubropertinctus].

The regulation of terephthalate catabolism was studied in Rhodococcus rubropertinctus which decomposed this synthetic monomer. The pathway (a) of terephthalate (TP) catabolism is as follows: TP----benzoate----4-hydroxybenzoate----protocatechuate----pyrocatechol-- --cycle ortho-cleavage. The following results were obtained when studying why two other catabolic pathways were realized if benzoate and 4-hydroxybenzoate were taken as a sole carbon source, namely, (b) benzoate----pyrocatechol----cycle cleavage and (c) 4-hydroxybenzoate----protocatechuate----cycle cleavage.

[Bacterial destruction of terephthalic acid and its isomers].

A strain of Mycobacterium lacticolum destructing the isomeric aryldicarbonic acids: teraphthalic, isophthalic and phthalic (in decreasing degree) has been selected from bacterial community of terephthalate containing industrial sewage biotreatment. The dominating role of M. lacticolum in microbial community increases during the continuous-flow cultivation under condition of terephthalate concentration increasing.

[Selection and biochemical activity of a microbial biocenosis in the process of concentrated sewage treatment].

A bacterial cenosis responsible for the destruction of organic wastes having a complex composition was selected under the conditions of continuous cultivation on highly concentrated industrial sewage. Most of the bacterial species and all of the yeasts and fungi were eliminated from the original microflora when the concentration of the purified sewage was increased from 2 to 12 g O2 per litre (in terms of the overall chemical oxygen uptake, COU) and the dilution rate (D) varied from 0.08 to 0.