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Thienylallylamines, readily accessible from the corresponding thienyl aldehydes, react with maleic and trifluoromethylmaleic anhydrides leading to the formation of acids with a thieno[2,3- f ]isoindole core. The reaction sequence involves two successive steps: acylation of the nitrogen atom of the initial allylamine and the intramolecular Diels-Alder vinylarene (IMDAV) reaction. The scope and limitations of the proposed method were thoroughly investigated. It has been revealed with the aid of X-ray analysis and DFT calculations that the key step, the IMDAV reaction, proceeds through an exo -transition state, giving rise to the exclusive formation of a single diastereomer of the target heterocycle. The obtained functionally substituted thieno[2,3- f ]isoindole carboxylic acids are potentially useful substrates for further transformations and bioscreening. The antimicrobial evaluation of the obtained compounds revealed that 1-oxo-2-(3-(trifluoromethyl)phenyl)hexahydrobenzo[4,5]thieno[2,3- f ]isoindole-10-carboxylic acid is the most active sample in the synthesized library. It exhibits antibacterial activity against sensitive strains of Gram-positive bacteria, including S. aureus , Enterococcus faecium , Bacillus cereus , and Micrococcus luteus , as well as the Gram-negative bacteria E. coli and Pseudomonas fluorescens , with MIC values ranging from 4 to 64 μg mL -1 . 9-Oxo-8-phenyloctahydronaphtho[2,1- d ]thieno[2,3- f ]isoindole-10-carboxylic acid showed antifungal activity against yeast culture C. albicans with a MIC value of 32 μM.

The antimicrobial activity and toxicity of three novel synthetic antibacterial agents containing tris (1 H -indol-3-yl)methylium fragment were studied in vitro and in vivo. All compounds in vitro revealed high activity (minimal inhibitory concentration (MIC) 0.13-1.0 µg/mL) against bacteria that were either sensitive or resistant to antibiotics, including multidrug-resistant clinical isolates. The derivatives combining high antimicrobial activity with relatively low cytotoxicity against human donor fibroblasts HPF-hTERT were subjected to further testing on mice. In vivo they revealed fairly good tolerance and relatively low toxicity. Acute toxicity was evaluated, and the main indicators of toxicity, including LD 50 and LD 10 , were determined. A study of compounds in vivo showed their efficiency in the model of staphylococcal sepsis in mice. The efficiency of compounds may be due to the ability of indolylmethylium salts to form pores in the cytoplasmic membrane of microbial cells and thereby facilitate the penetration of molecules into the pathogen.

The article describes a clinical case of myopericarditis as a late manifestation of possible COVID-19.

The microbial test-system based on cultivation of Halobacterium salinarum developed earlier for screening inhibitors of sterol biosynthesis and proposed for screening anticancer antibiotics, proved to be efficient in revealing anticancer compounds among derivatives of tris(1-alkylindol-3-yl)methylium, synthetic analogues of antibiotic turbomycin A. Most of the methane sulfonate and chloride salts of such compounds, investigated with the help of the H. salinarum test-system, showed no activity (MIC>32 mcM), while several derivatives, containing N-butyl or N-pentyl substituents were rather active against the bacterial strain. The MICs of them against H. salinarum were 8 mcM for total and 1 mcM for partial inhibition of the bacterial growth. The results of the study correlated with the results of other investigations that revealed anticancer activity of such compounds in tumor cell cultures. Therefore, the H. salinarum test-system demonstrated its availability for screening compounds with anticancer activity.

The aim of the research was to study clinical significance of "function-corrected" indexes (FCI) in non-invasive evaluation of aortic valvular stenosis (AVS) severity. 85 patients with degenerative aortic valve calcification (42 - with AVS and 43 - without aortic ostium (AO) stenosis) were subjects of a cross-sectional study. Significant correlation between AO area and FCI indexes was demonstrated. When it is not possible to determine AO by planimetric methods, it may be counted using FCI with good sensitivity (87%) and specificity (94%).

Atrial fibrillation (AF) is an independent risk factor for ischemic stroke. In patients with AF, cardioembolias present about 10% of ischemic strokes. Transesophageal echocardiography is an ideal instrument for diagnostics of intracardiac thrombi. An aim of the study was to find the high risk markers for stroke in patients with AF of non-valvular origin. The patients have been divided into 2 groups with and without stroke in anamnesis. To search for stroke dependence of clinical and echocardiographic high risk markers, the data were analyzed using Poly Analyst Power statistical package. In the group of the patients with stroke in the anamnesis, echocardiographic markers for high risk of thromboembolia occurred significantly more frequently. Thrombi in the left atrial or its appendage were registered in 12.5% patients without stroke in anamnesis and in 31% of those, who survived stroke. The independent risk factors for stroke were age, AF duration, left ventricular ejection fraction, diabetes mellitus and arterial hypertension.

A cyclodepsipeptide antibiotic 86/88 (enniatin B) with strong hypolipidemic action was isolated from the culture liquid of the fungus INA F-86/88 identified as Fusarium lateritium Nees var. stilboides (Wr.) Bilai. In the Hep G2 cell culture the antibiotic suppressed 14C-acetate incorporation into cholesterol (IC50 1.75 microM), cholesterol ethers (IC50 1 microM), triglycerides (IC50 1.3 microM) and free fatty acids (IC50 2.2 microM). The most pronounced effect of the drugs, i.e. the suppression of the cholesterol ethers synthesis is likely due not only to the ACAT inhibition but also to the inhibition of the triglyceride synthesis and the diminishing of the free fatty acids pool in the cells.

In the programme of screening of biologically active secondary metabolites produced by Streptomyces coeruleorubidus 2679 a new reddish-violet component (rubomycin Q1) with antibacterial and cytotoxic activity was isolated from the culture fluid of the organism. Some physico-chemical and biological properties of a chromatographically pure rubomycin Q1 were investigated. It was shown with the use of 1H NMR, UV, IR and mass spectrometry that rubomycin Q1 was an anthracycline antibiotic (9,10-anhydro-13-desoxycarminomycin).

Bleomycetin, an antitumor antibiotic, was subjected to chemical modification by the C-end fragment i.e. the residue of 3-[(4-aminobutyl)amino]propylamine (spermidine++) with acylation, carbamoylation and reducing alkylation, which yielded its new semisynthetic derivatives. The use of physicochemical methods showed that the chemical modification involved the primary and secondary amino groups++ of spermidine++ and gave rise to N,N'-diacyl, N,N'-dicarbamoyl and N,N'-dialkyl bleomycetins. The biological properties of the derivatives, i.e. their cytotoxic activity, acute and pulmonary toxicities were studied. The transformation of bleomycetin by the C-end fragment lowered the antibiotic toxicity and was believed to be a promising approach to modifying its molecule.