scholarly journals Synthesis and physical-chemical properties of (3-benzyl-8-propylxanthin-7-yl)acetohydrazide derivatives and their evaluation for antimicrobial and diuretic activities

Author(s):  
K. V. Aleksandrova ◽  
Ye. K. Mykhalchenko ◽  
O. S. Shkoda ◽  
D. A. Vasyliev

One of the most important tasks of our indigenous pharmaceutical science is the necessity for new medicines because existing drugs are characterized by various side effects, resistance, high toxicity, and so on. New bioactive molecule synthesis utilizes substances of natural origin as well as chemically modified ones. Thus, the researcher’s attention is mainly focused on 3-,7-,8-substituted derivatives of the natural heterocyclic xanthine system, which possess a wide range of pharmacological action. Synthesis of a novel of (3-benzyl-8-propylxanthin-7-yl)acetohydrazides with antimicrobial and diuretic activities described in the paper. The aim of this work is to develop efficient methods for synthesis of (3-benzyl-8-propylxanthin-7-yl)acetohydrazide derivatives, and to study their physical-chemical properties. Materials and methods. Two-hour boiling of propyl 2-(3-benzyl-8-propylxanthine-7-yl)acetate by excess hydrazine hydrate in propan-2-ol medium have yielded the key the key intermediate 2-(3-benzyl-8-propylxanthine-7-yl)acetohydrazide. Further transformation of the latter has led to formation of corresponding acetohydrazide derivatives achieved by the reaction with aliphatic, aromatic, heterocyclic aldehydes, and ketones. The structure and the relative configuration of the synthesized compounds were elucidated by analyzing their physical-chemical data. Results. The synthesis and optimization of reaction conditions of (3-benzyl-8-propylxanthin-7-yl)acetohydrazide derivatives were conducted. The identification of all synthesized compounds was aided by various physical-chemical methods (thin layer chromatography, elemental analysis, IR, and 1H NMR spectroscopy). Conclusions. As a result of synthetic research the preparative synthesis method of (3-benzyl-8-propylxanthin-7-yl)acetohydrazide derivatives possessing antimicrobic, and diuretic activities was developed.

Author(s):  
Cristina Mihali ◽  
◽  
Ionut Grad ◽  
Thomas Dippong ◽  
◽  
...  

The aim of this study was to evaluate the physical-chemical characteristics of different types of coffee, decaffeinated and of two types of coffee substitutes based on barley and chicory. The following physical-chemical characteristics were performed: moisture, pH, content of polyphenols and qualitatively determination of caffeine, by thin-layer chromatography. The moisture of the investigated coffee and substitutes of coffee was in the range 1,5 and 3,6%. By analyzing the moisture of the coffee substitutes, we observed that coffee based on barley has the highest moisture and chicory has the lowest value. The caffeine was qualitatively determined by thin-layer chromatography. It was found that all types of the investigated samples contain caffeine excepting decaffeinated coffee. Polyphenols content of the analysed coffee samples varied in the range of 2.8-3.2 mg/g.


Materials ◽  
2019 ◽  
Vol 12 (13) ◽  
pp. 2199
Author(s):  
Junhai Wang ◽  
Ting Li ◽  
Tingting Yan ◽  
Xiaoyi Wei ◽  
Xin Qu ◽  
...  

In this study, we use an aqueous solution synthesis method to prepare silver perrhenate powders and suspend them into a poly alpha olefin (PAO) base oil with polyoxyethylene octylphenyl ether. Four ball tests and ball-on-disk reciprocating mode are performed to determine how silver perrhenate performs tribologically as a lubricating additive over a wide range of temperatures. The physical and chemical properties, as well as the lubricating mechanisms of the silver perrhenate additive, are characterized via X-ray diffraction, scanning electron microscope, Fourier transformation infrared spectroscopy, Raman spectrum, and X-ray photoelectron spectroscopy. The four-ball test results demonstrate that the oil added with silver perrhenate additive is more effective than the base oil in reducing friction and improving wear resistance, and provides the best lubricating performance when at a concentration of 0.5 wt%. The reciprocating mode findings indicate that the hybrid lubricant exhibits distinctively better tribological properties than the base oil at high temperatures, and its low shear strength and chemical inertness allow for low friction at elevated temperatures. The resulting silver perrhenate layer that incorporates native superalloy oxides on the worn surface can provide lubrication by serving as a barrier that prevents direct contact between the rubbing surfaces at elevated temperatures.


1986 ◽  
Vol 21 (3) ◽  
pp. 344-350 ◽  
Author(s):  
Barry G. Oliver ◽  
Klaus L.E. Kaiser

Abstract The concent rat ions of hexachloroethane (HCE), hexachlorobutadiene (HCBD), pentachlorobenzene (QCB), hexachlorobenzene (HCB) and octachlorostyrene (OCS) in large volume water samples show that the major sources of these chemicals to the St. Clair River are Dow Chemical Company effluents and, to a lesser degree, Sarnia’s Township ditch which drains one of Dow’s waste disposal sites. Tributaries entering the river on both sides of the Canada/United States border contain measurable concentrations of these chemicals indicating low level contamination throughout the area. The degree of water/suspended sediment partitioning of the chemicals (Kp) was studied. Kp values for the individual chemicals changed in a manner consistent with changes in their physical-chemical properties.


2020 ◽  
Vol 20 (11) ◽  
pp. 1340-1351 ◽  
Author(s):  
Ponnurengam M. Sivakumar ◽  
Matin Islami ◽  
Ali Zarrabi ◽  
Arezoo Khosravi ◽  
Shohreh Peimanfard

Background and objective: Graphene-based nanomaterials have received increasing attention due to their unique physical-chemical properties including two-dimensional planar structure, large surface area, chemical and mechanical stability, superconductivity and good biocompatibility. On the other hand, graphene-based nanomaterials have been explored as theranostics agents, the combination of therapeutics and diagnostics. In recent years, grafting hydrophilic polymer moieties have been introduced as an efficient approach to improve the properties of graphene-based nanomaterials and obtain new nanoassemblies for cancer therapy. Methods and results: This review would illustrate biodistribution, cellular uptake and toxicity of polymergraphene nanoassemblies and summarize part of successes achieved in cancer treatment using such nanoassemblies. Conclusion: The observations showed successful targeting functionality of the polymer-GO conjugations and demonstrated a reduction of the side effects of anti-cancer drugs for normal tissues.


2020 ◽  
Vol 10 (3) ◽  
pp. 169-184
Author(s):  
Rachna Anand ◽  
Arun Kumar ◽  
Arun Nanda

Background: Solubility and dissolution profile are the major factors which directly affect the biological activity of a drug and these factors are governed by the physicochemical properties of the drug. Crystal engineering is a newer and promising approach to improve physicochemical characteristics of a drug without any change in its pharmacological action through a selection of a wide range of easily available crystal formers. Objective: The goal of this review is to summarize the importance of crystal engineering in improving the physicochemical properties of a drug, methods of design, development, and applications of cocrystals along with future trends in research of pharmaceutical co-crystals. Co-crystallization can also be carried out for the molecules which lack ionizable functional groups, unlike salts which require ionizable groups. Conclusion: Co-crystals is an interesting and promising research area amongst pharmaceutical scientists to fine-tune the physicochemical properties of drug materials. Co-crystallization can be a tool to increase the lifecycle of an older drug molecule. Crystal engineering carries the potential of being an advantageous technique than any other approach used in the pharmaceutical industry. Crystal engineering offers a plethora of biopharmaceutical and physicochemical enhancements to a drug molecule without the need of any pharmacological change in the drug.


2019 ◽  
Vol 5 (4) ◽  
pp. 270-277 ◽  
Author(s):  
Vijay Kumar ◽  
Simranjeet Singh ◽  
Ragini Bhadouria ◽  
Ravindra Singh ◽  
Om Prakash

Holoptelea integrifolia Roxb. Planch (HI) has been used to treat various ailments including obesity, osteoarthritis, arthritis, inflammation, anemia, diabetes etc. To review the major phytochemicals and medicinal properties of HI, exhaustive bibliographic research was designed by means of various scientific search engines and databases. Only 12 phytochemicals have been reported including biologically active compounds like betulin, betulinic acid, epifriedlin, octacosanol, Friedlin, Holoptelin-A and Holoptelin-B. Analytical methods including the Thin Layer Chromatography (TLC), High-Performance Thin Layer Chromatography (HPTLC), High-Performance Liquid Chromatography (HPLC) and Liquid Chromatography With Mass Spectral (LC-MS) analysis have been used to analyze the HI. From medicinal potency point of view, these phytochemicals have a wide range of pharmacological activities such as antioxidant, antibacterial, anti-inflammatory, and anti-tumor. In the current review, it has been noticed that the mechanism of action of HI with biomolecules has not been fully explored. Pharmacology and toxicological studies are very few. This seems a huge literature gap to be fulfilled through the detailed in-vivo and in-vitro studies.


2021 ◽  
Vol 11 (10) ◽  
pp. 4417
Author(s):  
Veronica Vendramin ◽  
Gaia Spinato ◽  
Simone Vincenzi

Chitosan is a chitin-derived fiber, extracted from the shellfish shells, a by-product of the fish industry, or from fungi grown in bioreactors. In oenology, it is used for the control of Brettanomyces spp., for the prevention of ferric, copper, and protein casse and for clarification. The International Organisation of Vine and Wine established the exclusive utilization of fungal chitosan to avoid the eventuality of allergic reactions. This work focuses on the differences between two chitosan categories, fungal and animal chitosan, characterizing several samples in terms of chitin content and degree of deacetylation. In addition, different acids were used to dissolve chitosans, and their effect on viscosity and on the efficacy in wine clarification were observed. The results demonstrated that even if fungal and animal chitosans shared similar chemical properties (deacetylation degree and chitin content), they showed different viscosity depending on their molecular weight but also on the acid used to dissolve them. A significant difference was discovered on their fining properties, as animal chitosans showed a faster and greater sedimentation compared to the fungal ones, independently from the acid used for their dissolution. This suggests that physical–chemical differences in the molecular structure occur between the two chitosan categories and that this significantly affects their technologic (oenological) properties.


2020 ◽  
Vol 59 (1) ◽  
pp. 441-454
Author(s):  
Carlos A. Martínez-Pérez

AbstractIn the last years, electrospinning has become a technique of intense research to design and fabricate drug delivery systems (DDS), during this time a vast variety of DDS with mainly electrospun polymers and many different active ingredient(s) have been developed, many intrinsic and extrinsic factor have influence in the final system, there are those that can be attributed to the equipment set up and that to the physical-chemical properties of the used materials in the fabrication of DDS. After all, this intense research has generated a great amount of DDS loaded with one or more drugs. In this manuscript a review with the highlights of different kind of systems for drug delivery systems is presented, it includes the basic concepts of electrospinning, types of equipment set up, polymer/drug systems, limitations and challenges that need to be overcome for clinical applications.


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