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  • Open access
  • 90 Reads

Twenty five novel imidazole analogs 2(a-r) & 3 (a-g) were designed, based on QSAR studies. The designed compounds were subjected to molecular docking studies and predictive ADME studies were performed. Molecular docking studies were performed in the active site of HIV-1-reverse transcriptase PDB ID: 1RT2 & glucosamine-fructose-6-phosphate animotransferase PDB ID: 2VF5. AutoDock tools v1.5.6 was used for the molecular docking studies. The binding mode analysis of the compounds was done. Docking studies suggested that all the compounds showed good interactions i.e, H-bonding interactions and pi-pi interactions when compared to the standard compounds i.e, nevirapine (in case of PDB ID:1RT2) and metronidazole (in case of PDB ID:2VF5). The predictive ADME studies also showed that all the compounds have drug-like properties. The results show that these compounds can be synthesised and further explored for their possible antimicrobial and antiviral activities.

  • Open access
  • 59 Reads
An original method for the synthesis of partially deuterated natural lembehyne B and the study of its biological activity.

An efficient method for the synthesis of a partially deuterated analogue of the natural neuritogenic alkynol, lembehyne B, has been developed for the first time, based on the use of a new reaction of Ti-catalyzed cross-cyclomagnesiation of O-containing 1,2-dienes and terminal aliphatic 1,2-dienes using EtMgBr in high yield. The introduction of two deuterium atoms is carried out at the stage of treatment of the formed in situ magnesacyclopentane with D2O.

  • Open access
  • 24 Reads
An original method for the synthesis and the study of its biological activity of natural lembehyne B aromatic analogs.

In the development of earlier initiated studies on the synthesis of natural and synthetic neuritogenic alkynols, lembehynes A-C, which, simultaneously, exhibit high antitumor activity, we have developed a method for the synthesis of an analogue of natural lembehyne B containing a phenyl radical in its structure. It has been shown that the synthesized aromatic analogue of lembehyne B exhibits higher antitumor activity in vitro to a number of tumor cell lines (Jurkat, K562 and U937).

  • Open access
  • 44 Reads
Natural and synthetic dienoic and trienoic acids - an original method for the synthesis and antitumor activity.

The report contains the recent data about our research on the synthesis and study of the properties of unique natural and synthetic Z,Z-dienoic and Z,Z,Z-trienoic fatty acids exhibiting a wide range of biological activities (antiviral, antibacterial, neuritogenic, antitumor, antiparasitic, fungicidal). All the methods and approaches for the synthesis of the above-mentioned unsaturated carboxylic acids presented in the report are based on the using at the key stage of the synthesis of the catalytic cross-cyclomagnesiation of 1,2-dienes developed by the main co-authors.

  • Open access
  • 133 Reads
Azide-Alkyne Cycloaddition Catalyzed by a Glucose/Benedict Reagent System

Benedict's Reagent is commonly used in identifying reducing sugars through a redox process where a Cu(I) species is generated. Despite the simplicity of this reaction, this has barely been investigated as a copper (I) source for catalytic processes. In this report, diverse organic azides and alkynes were reacted in presence of catalytic amounts of a Glucose-Benedict Reagent system, obtaining the corresponding 1,2,3-triazoles through a simple and environmentally friendly synthetic procedure.

  • Open access
  • 72 Reads
Study the effect of applying benzimidazole-ethanol solution as a film-forming corrosion inhibitor on the surface of aluminium alloy 2024-t3
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The Al-Cu-Mg light alloys storage such that their use for building structural, marine offshore, and aeroplane components with excellent strength/weight ratios would not be possible without adherent anti-corrosion preservation. Many techniques and strategies are still being used to treat the surface, such as cladding, anodizing, and greasing. However, due to the cost, time consumed, and processing these techniques is considered complicated. Therefore, applying volatile organic inhibitors components are now being used effectively. Benzimidazole (BZI) and its derivatives are one of these film-forming chemicals used on copper and steel directly or as injectable combined with other carriers such as fatty acids or dissolvable hydrocarbons with high efficiency on corrosion protection. Therefore, this paper will investigate the enhancement of the corrosion protection afforded by direct spraying of BZI solution on the surface of aluminium alloy 2024-t3. The corrosion protection performance results from the high electro-negativity of BZI and as a film-forming inhibitor, which will be adsorbed on the metallic surface as it may emulate the active protection. The corrosion protection properties of the BZI film-forming coating were preliminary studied within 3.5% NaCl by using electrochemical impedance testing and simulations. The surface chemical adsorption confirmation was done by infrared spectroscopy (ATR-FTIR), supported by analyzing the morphology of the surface before and after the immersion testing by using scanning electron microscopy (SEM) and real-image within one week of immersion. The Benzimidazole film-forming coating exhibited good anti-corrosion properties, providing an adherent protection film on AA 2024-t3 samples comparing to cladded bare AA2024-t3 with a cost-effective and easy applying process.

  • Open access
  • 59 Reads
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Royal jelly (RJ) is one of the most popular beehive products, also labeled as a superfood because of its complex composition. It has been traditionally used as dietary supplement and possess several confirmed pharmaceutical properties. Its anticancer potential has been mainly attributed to unsaturated fatty acid 10H2DA, present only in RJ and not found elsewhere in nature. The present study aimed to evaluate content of 10H2DA in the RJ sample (originated from Serbia) using HPLC method. Furthermore, the potential of this unique RJ compound in suppressing motility of colorectal carcinoma cells (HCT-116, SW-480) was assessed by Transwell assay. Cells were treated with two selected sublethal concentrations (10 and 100 μM) for 24 h. Our results showed that the tested RJ sample contained 9.22±0.02 mg/g (0.92% w/w) of 10H2DA, and obtained result is in accordance to the literature data of 10H2DA in RJ in the range of 0.8%-6.5%. Meanwhile, 10H2DA in both concentrations significantly reduced motility of HCT-116 cells. However, the migratory potential of the SW-480 cells remained almost unchanged when treated with 10H2DA. Obviously, tested substance was able to inhibit motility of more aggressive HCT-116 cells than less mobile SW-480 cell line, which is a significant result of our study, and indicating stronger sensitivity of HCT-116 cells to the treatment.

This is the first report of 10H2DA content in RJ sample from Serbia, as far as we know. Due to its significant antimigratory effect on aggressive colorectal carcinoma cells, 10H2DA presents promising agent for future studies concerrning anticancer treatment.

  • Open access
  • 63 Reads
Synthesis and molecular docking of N,N'-[succinylbis(oxy)]dibenzamides as inhibitors of Cathepsin S and Cathepsin K.

The reaction of interaction of benzhydroxamic and 4-nitrobenzhydroxamic acids with succinic acid chloride, carried out in an acetonitrile medium during boiling, has been studied. It was revealed that the result of the reaction is the formation of N,N'-[succinylbis(oxy)]dibenzamides, the structure of which was proved by 1H, 13C NMR. Using the online program PASS, the biological activity of the obtained compounds was predicted. It was found that N,N'-[succinylbis(oxy)]dibenzamides can inhibit cathepsins (enzymes that degrade protein) with a high probability. Using the online program Mcule, molecular docking of the obtained dibenzamides and their analogs with Cathepsin S, Cathepsin K was carried out, and ligands with the highest affinity for the Cathepsin family were identified. Using the Hyperchem program, semiempirical methods were used to analyze the possibility of synthesizing suitable ligands.