Among all modern antibiotics, fluoroquinolones are well known for their broad spectrums of activity and efficiency toward microorganisms and viruses. However, antibiotic resistance is still a problem, which has encouraged medicinal chemists to modify the initial structures in order to combat resistant strains. Our current work is aimed at synthesizing novel hybrid derivatives of ciprofloxacin and norfloxacin and applying docking studies and biological activity evaluations in order to find active promising molecules. We succeeded in the development of a synthetic method towards 1,2,3-triazole-substituted ciprofloxacin and norfloxacin derivatives. The structure and purity of the obtained compounds were confirmed by 1H NMR, 13C NMR, 19F NMR, LC/MS, UV-, IR- spectroscopy. Docking studies, together with in vitro research against Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Bacillus subtilis ATCC 6633, Pseudomonas aeruginosa ATCC 27853, Candida albicans NCTC 885-653 revealed compounds in which activity exceeded the initial molecules.
The aim of the work. Among all the representatives of four generations of fluoroquinolones ciprofloxacin (CIPRO) and norfloxacin (NOR) remain widely used and prescribed antibiotics in clinical practice. However, the problem of resistance towards them is gradually increasing. Thus, our investigation is dedicated to chemical modification of C-7 position of Ciprofloxacin and Norfloxacin ring as a promising solution to combat antibiotic resistance and open a pathway towards convenient synthesis of new fluoroquinolones derivatives. Materials and methods. The subjects of the research were N-piperazine-substituted ciprofloxacin and norfloxacin. The methods of molecular docking and organic synthesis were applied in the study. The structures of the obtained compounds were confirmed by 1H NMR, 13C NMR, 19F NMR, LC/MS, IR, UV spectroscopy. The antimicrobial activity was measured by the method of double serial dilutions against Staphylococcus aureus (ATCC 25923), Escherichia coli (ATCC 25922), Bacillus subtilis (ATCC 6633), Pseudomonas aeruginosa (ATCC 27853), Candida albicans (NCTC 885-653) and diffusion in agar method against clinical strains. The results. 7-(4-(2-Cyanoacetyl)piperazin-1-yl)-1-R-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acids were synthesized and their structures were confirmed. The obtained compounds showed the antibacterial activity on the reference level for double dilution method and exceeded control for “well” method. Conclusions. The current investigation revealed the promising route for the expanding of the existing fluoroquinolones diversity. Pharmacodynamics and pharmacokinetics changes could be achieved by chemical modifications of C-7 position of the initial ring. Further research utilizing the obtained compounds as starting ones opens a promising way to novel active molecules synthesis and combating the problem of antibiotic resistance
Sapropel muds have a different chemical composition and provide the anti-inflammatorySapropel muds, which have a unique composition, effectively affect the functions of the whole organism and, especially the skin. They possess the anti-inflammatory, anti-allergic action, protect the skin from destructive effects of free radicals, give it elasticity, firmness and freshness. They also moisten the horny layer of the epidermis, and improve cellular regeneration [4].Cosmetic products on the basis of sapropel are presented by different forms, but the most often in the form of masks (37.10%) and the natural raw material (15.70%) [5]. Masks are products of an intensive effect, and it causes exactly the spread of masks among the preparations of sapropel considering the diversity of the chemical composition and the pharmacological and cosmetic effects. To provide masks with plasticity and better organoleptic properties (elimination of a specific soil odour, the presence of small particles, the residues of plant life), as well as to expand the range of sapropel masks with the various pharmacological action (lifting, anti-cellulite, antiseborrheic and anti-acne effect, etc.) it was proposed to use one of the products of sapropel -the sapropel paste for the base of masks.The sapropel paste is a paste-like product of the natural origin made of the lake sapropel, it contains biologically active substances, and the complex of macroand microelements [6].By appearance the sapropel paste is a homogenous pasty mass of a dark brown colour with pH -6.7, the moisture content -83%, and the content of organic substances -76.63% [6].However, the sapropel paste is a medium for development of microorganisms, including anaerobic ones. Therefore, the aim of our study was to substantiate experimentally the choice of an effective preservative in the composition of cosmetic masks with the sapropel paste to prevent microbiological contamination and ensure their stability. Materials and MethodsThe objects of the research were experimental samples of the sapropel paste taken from the Prybych deposit of the Volyn region: Sample 1 (paste of sapropel); Sample 2 (paste of sapropel, 0.1% of nizin); Sample 3 (paste of sapropel, 0.01% of nizin, 0.8% of germaben); Sample 4 (paste of sapropel, 0.01 of nizin, 0.1% of euxyl K 100).The experimental samples of the sapropel paste obtained from the sapropel powder (the dry anhydrous product obtained from the native (natural) sapropel) and water by the method of cavitation with the speed from 100 to 3500 rpm for 30 min at the temperature of 50°C. Then they were cooled to the temperature of 35-40°C, and the preservatives were added.For the sapropel paste the structural and mechanical (rheologic) parameters were determined according to the requirements of the SPhU (1.0, 2.2.10). The studies were carried out on a Brookfild HB DV-PRO ΙΙ rotatory viscometer (USA) using the adapter of the rotatory type with coaxial cylinders (the spindle SS4-21 for the chamber with the volume of 8.3 g) in the range of the gradient of t...
Purpose of the study: to investigate the impact of hydroxyethyl starch (HES) and polyethylene oxide (PEO) on the indicators of preservation of murine testis interstitial cells (IC) under cryopreservation.Materials and methods. To isolate IC the enzymes were used: 0.2 mg/ml collagenase and 0.1 mg/ml DNase. The obtained cell suspension was cryopreserved in the solutions that contained 0; 0,7; 1,4; 2,1; 2,8 M of dimethyl sulfoxide (DMSO) and/or 10%, 20% fetal cow serum, 10 mg/ml PEO or HES. The samples (1 ml) were cooled at a rate of 1 °C/min to -80 °C then stored in liquid nitrogen (-196 °C). They were warmed at 37 °C in the water bath. Cryopreservation solution was removed. The number of cells and their preservation were assessed before and after with the assistance of Goryaev’s camera. Viability of IC, Leydig cell preservation and preservation of metabolic activity were measured with trypan blue dye, histochemical staining for 3β-hydroxysteroid dehydrogenase activity.Results. It was shown that 1,4 M DMSO without supplements favored IC preservation. Addition to the cryopreservation solution 10% and 20% of fetal cow serum or 10 mg/ml HES increased total preservation of IC by more than 10% and Leydig cell cryopreservation by an average 15%. HES 10 mg/ml may decrease DMSO concentration to 0,7 M. This combination had the best indicators of total preservation of IC, preservation of viable cells and Leydig cells: 75,8 (53,3; 93,3), 55,6 (45,1; 69,4), 57,1 (40,2;70,3) %, respectively. PEO was ineffective.Conclusion. High-molecular weight synthetic polymers such as HES can substitute protective properties of blood serum under cryopreservation and allow decreasing effective concentration of permeable cryoprotective such as DMSO.
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