Synthesis and Antibacterial Activity of New 6″-Modified Tobramycin Derivatives.

Aminoglycosides are one of the first classes of natural antibiotics which have not lost relevance due to their broad spectrum of action against Gram-positive, Gram-negative bacteria and mycobacteria. The high growth rate of antimicrobial resistance (AMR) together with the severe side effects of aminoglycosides increase the importance of developing improved semisynthetic derivatives. In this work, we proposed a synthetic route to new tobramycin derivatives modified at the 6″-position with aminoalkylamine or guanidinoalkylamine residues.

Triphenylphosphonium Analogs of Short Peptide Related to Bactenecin 7 and Oncocin 112 as Antimicrobial Agents.

Antimicrobial peptides (AMPs) have recently attracted attention as promising antibacterial agents capable of acting against resistant bacterial strains. In this work, an approach was applied, consisting of the conjugation of a peptide related to the sequences of bactenecin 7 (Bac7) and oncocin (Onc112) with the alkyl(triphenyl)phosphonium (alkyl-TPP) fragment in order to improve the properties of the AMP and introduce new ones, expand the spectrum of antimicrobial activity, and reduce the inhibitory effect on the eukaryotic translation process. Triphenylphosphonium (TPP) derivatives of a decapeptide RRIRPRPPYL were synthesized.

Synthesis of 6″-Modified Kanamycin A Derivatives and Evaluation of Their Antibacterial Properties.

Aminoglycosides are one of the first classes of antibiotics to have been used clinically, and they are still being used today. They have a broad spectrum of antimicrobial activity, making them effective against many different types of bacteria. Despite their long history of use, aminoglycosides are still considered promising scaffolds for the development of new antibacterial agents, particularly as bacteria continue to develop resistances to existing antibiotics.

Diversity, novelty, antimicrobial activity, and new antibiotics of cultivable endophytic actinobacteria isolated from psammophytes collected from Taklamakan Desert.

Three hundred and twenty endophytic actinobacterial strains were isolated from psammophytes collected from Taklamakan Desert and identified. Among them, three strains already had been identified as new species of two genera and sixteen isolates showed relatively low 16S rRNA similarities < 98.6% to validly described species.

The lanthanide complexes of 2,2'-bipyridyl-6,6'-dicarboxylic dimethylanilides: the influence of a secondary coordination sphere on the stability, structure, luminescence and f-element extraction.

Four of the six possible isomeric 2,2'-bipyridyl-6,6'-dicarboxylic dimethylanilides were studied from the point of view of the impact of a secondary coordination sphere on the formation of complexes with lanthanides in solution, as well as the crystal structure and photophysical properties of the complexes. All ligands form complexes with a 1 : 1 metal-to-ligand ratio with an lg β1 in the range of 6.0-8.

Structure of Francisella tularensis peptidyl-tRNA hydrolase.

The rational design of novel antibiotics for bacteria involves the identification of inhibitors for enzymes involved in essential biochemical pathways in cells. In this study, the cloning, expression, purification, crystallization and structure of the enzyme peptidyl-tRNA hydrolase from Francisella tularensis, the causative agent of tularemia, was performed. The structure of F.

[Use of beta-methyldigoxin preparations medilazine and bemecor in patients with congestive heart failure].

The two agents beta-methyldigoxin (medixin), a Soviet medilazide, and bemecor (digicor), a foreign analogue (LEK, Yugoslavia) were comparatively evaluated. An equal high (85%) clinical efficacy of the drugs was found in 81 patients with varying stages of heart failure. A positive therapeutic effect was accompanied by lower heart rate, higher diuresis and natri-and kaliuresis, decreased systolic and diastolic pressures in the pulmonary artery.

[Intracavity thermo- and gamma-therapy of uterine cancer].

Some methodological problems of the use of intracavitary UHF hyperthermia combined with intracavitary gamma-beam therapy in combined radiation therapy of uterine cancer patients are considered. Indications for the use of this method and radiobiological substantiation of thermoradiotherapy for this group of patients are discussed. The advantages of the proposed method of thermoradiotherapy have been noted on the basis of immediate clinical observations, endoscopic, x-ray and morphometric findings.

[Use of high doses of glucocorticoids in patients with rheumatic diseases].

Short-term application of high doses of glucocorticoids removes the acuity of the generalized patterns of systemic rheumatic diseases. This is documented by the reported data and analysis of the authors' own 15 observations. The dose of glucocorticoids, duration of their application and administration routes are determined by the degree of the pathological process activity and by the organs concerned (kidneys, central nervous system).

[Use of the aldosterone antagonist, canrenoate potassium for treating chronic circulatory insufficiency].

The results of studying the clinical effect of the diuretic soldacton and its effect on a number of indices of water-electrolyte metabolism are discussed. The drug was used in 16 patients with IIB--III stage of circulatory insufficiency. It was found that soldacton possesses a moderate diuretic and natriuretic effect and produces a potassium-preserving effect.

[Content and distribution of water and potassium in the body of patients with chronic circulatory insufficiency].

The total water content (after antipyrine and tritium oxide), that of extracellular water (after sodium thiosulphate) and of overall metabolic potassium (with reference to K42) were studied concurrently in 34 patients with chronic circulatory insufficiency. Twenty normal subjects served as controls. In the sick the disturbances of the water metabolism made themselves felt not only in the accumulation of surplus water in the body, but also in its re-distribution.