Transition metal complexes with heteroaromatic ligands offer a promising strategy for developing novel anticancer agents. In this study, the ligand 12-hydroxy-7-iminocromeno[4,3-d]pyrido[1,2-a]pyrimidin-6(7H)-one was used to synthesize new cobalt(II), nickel(II), and titanium(III/IV) complexes via conventional and microwave-assisted methods, with the latter providing higher yields and shorter reaction times. The complexes were characterized by FT-IR, 1H- and 13C-NMR, mass spectrometry, and elemental analysis, confirming coordination through the azomethine nitrogen and phenolic oxygen atoms. Their in vitro antiproliferative activity was evaluated against the H460, MCF-7, and HCT116 human cancer cell lines, with doxorubicin used as a positive control. Cytotoxicity was expressed as GI50 values. All complexes exhibited moderate to pronounced antiproliferative effects. The nickel(II) and cobalt(II) complexes showed moderate activity, whereas the titanium(III/IV) complexes were the most potent, displaying significantly higher cytotoxicity than the free ligand, with GI50 values in the low micromolar range. These findings highlight the influence of the metal center on biological activity and identify the titanium complexes as promising candidates for further anticancer studies.
In recent years, the requirements for the use of herbal products and formulations against the solar radiation have increased, trying to avoid the excesive use of chemicals considered harmful to human health. The aim of this study was to determine the value of the sun protection factor (SPF) from the plant extracts of Achillea millefolium L. using solvents of different polarity such as ethanol, ethyl acetate and hexane. Determination of the SPF value of plant extracts was carried out by UV-Vis spectrophotometer measurements in the region of ultraviolet radiation, in the range of wavelengths 290-320 nm. From the obtained results it has been observed that all the extracts show protective ability against ultraviolet radiation. The highest SPF value of 35.5 was obtained fromA. A. millefolium L. extracts with ethyl acetate extracted by Soxhlet extraction. While A. millefolium L. extracts with hexane, extracted with cold extraction, showed the lowest SPF value of 8.06. From the results achieved, we have estimated that the plant A. millefolium L. has high photoprotective potential and as such its extracts can be used in sunscreen formulations. The spectrophotometric method used is fast, simple and cost-effective for the in vitro determination of SPF values.
The purpose of this paper is the synthesis of new metal complexes and their biological application. Four new transition metal complexes (2-5) were synthesized using conventional as well as microwave methods from 7-iminochromeno[4,3-d]pyrido[1,2-a]pyrimidin-6(7H)-one (1) and corresponding metal salts. Ligand 1 and metal complexes 2-5 were characterized by IR, 1H-NMR, 13 C-NMR, Mass spectroscopy and elemental analysis. The free ligand and the metal complexes have been tested for in vitro antiproliferative activity. The evaluation of the antiproliferative effects of compounds (1-5) on three tumor cell lines (H460, MCF-7, and HCT116) shows that all tested compounds have demonstrated moderate to pronounced antiproliferative and/or cytotoxic effect. The most active compounds were ligand 1 and metal complexes 3 and 5.
The aim of this study was determination of heavy metals: copper, cadmium, lead and zinc, in honey as a bio monitor for environmental pollution. We analyzed multifloral honey samples from six different localities from Kosovo, where four of them were from industrial places (Obiliq, Palaj, Kline and Volljake), and two others (Dragash and Rugove) from nonindustrial places. Investigation of heavy metals in honey was conducted by Atomic Absorption Spectrometry (AAS).The most present from selected heavy metals in honey was zinc ranged from 2.81-6.73 mg/kg, copper 0.32-0.70 mg/kg, and leadranged from 0.04-0.352 mg/kg, while concentrations of cadmium were below limit detection of method used. Honey samples analyzed were not free from heavy metals, but these values were below the maximum concentrations of heavy metals in different foods recommended by FAO/WHO.
Two novel ligands 7‐iminochromeno[4,3‐d]pyrido[1,2‐a]pyrimidin‐6(7H)‐ones have been prepared. The ligands and their Co(II) metal complexes have been characterized by IR, 13C‐NMR, 1H‐NMR, Mass spectra and Elemental analysis. Antimicrobial activities of the ligands and their complexes have been screened against the Escherichia coli ATTC 8739 and Staphylococcus aureus ATTC 25923. The results show that Co (II) complexes possess higher antibacterial activities than ligands towards the bacterial species.
This study presents the synthesis of 7‐iminobenzo[b]chromeno[4,3‐e][1,4]diazepin‐6(7H)‐ones (3–4) by simple reaction of 4‐chloro‐2‐oxo‐2H‐chromene‐3‐carbonitrile with o‐phenylidenediamine. The compounds (3–4) were characterized by elemental analysis data, IR, 1H NMR and mass spectral data. The novel heterocyclic compounds were evaluated for antimicrobial activity against Escherichia coli and Staphylococus aureus using the Kirby‐Bayer method. The novel compounds demonstrated moderate antimicrobial activity.Support or Funding InformationFunding: Support for this study was provided by the Ministry of Education, Science and Technology of the Republic of Kosovo. Grant number:2‐5521‐2This abstract is from the Experimental Biology 2019 Meeting. There is no full text article associated with this abstract published in The FASEB Journal.
A wild plant (Sanguisorba albanica) from Kosovo exhibits an appealing aroma, which was perceived as intensely fresh, green, and slightly sweetish with hints of cucumber, melon, and green tea. The characteristic aroma of S. albanica was analyzed for the first time by employing advanced molecular sensory techniques coupled with multiple headspace solid phase microextraction (MHS-SPME). Thirty-six different odor impressions were perceived, and 34 corresponding compounds were identified by a gas chromatography system equipped with a mass spectrometric detector and an olfactory detection port. By aroma dilution analysis, sixteen key odorants with flavor dilution factors higher than 16 were identified. Their respective concentrations were quantified by means of MHS-SPME according to the determined β values (0.43–0.83), and odor activity values (OAVs) were calculated. (E,Z)-2,6-Nonadienal (green, melon-like, and sweetish odor; OAV 20,046), followed by linalool (floral and citrus-like odor; OAV 10,563), (Z)-6-nonenal (cucumber-like, green, and melon-like odor; OAV 4200), ethyl isobutyrate (floral and fruity odor; OAV 1315), and (E)-2-nonenal (green and fatty odor; OAV 1062) were representative odorants contributing to the overall aroma of S. albanica. Differences between stems, leaves, and flowers of S. albanica with regard to the key odorants were also presented. Intensely green and floral aromas of the leaves and flowers were greatly attributed to (E,Z)-2,6-nonadienal and linalool, respectively. Apart from these compounds, (Z)-6-nonenal contributed to the overall aroma of the stems as well.
New complexes of 2‐Oxo‐2H‐Chromene‐3‐Carbonitrile with cobalt [Co (II)], nickel [Ni(II)], iron [Fe(III)] and chromium [Cr(III)] were synthesized. The structure of synthesized compounds were characterized by IR, 1H‐NMR and elemental analysis. The synthesized ligand and metal complexes were screened for microbiological activity against Escherichia coli Staphylococcus aureus, and Klebsiella pseumoniae. The complexes have enhanced activity compared to the 4‐Hydroxy‐2‐Oxo‐2H‐Chromene‐3‐Carbonitrile itself as ligand.Support or Funding InformationSupport for this study was provided by the Ministry for Education, Science and Technology of the Republic of Kosovo. Grant number:2‐5521‐2This abstract is from the Experimental Biology 2018 Meeting. There is no full text article associated with this abstract published in The FASEB Journal.
Sediment transport is one of the most powerful factor on river hydrology. It has vital importance for water engineering projects. There are many sediment transport formulas in the literature but most of them are derived from small data sets of natural rivers or experimental designs. Each formulation has its own restrictions, which depends on the original dataset of that study. None of them have gained universal acceptance. As a result, investigation towards the development of more accurate and simpler formulae is still necessary and should be continued.
Current study based on the synthesis of new 1,2,4‐triazole compounds containing purine moiety: 9H‐[1,2,4]triazolo[4,3‐g] purin‐5‐amine I and 5‐amino‐3H‐[1,2,4]triazolo[4,3‐g]purine‐3‐thione II.Synthesized compounds were characterized by IR,NMR, and elemental analysis. The synthesized compounds have been screened for in vitro antibacterial activity against Staphylococcus aureus ATCC 25923 Escherichia coli ATCC 25922 and Klebsiella pneumonie PR 23/07 by cup plate method at concentrations 1,3,5 mg/ml. DMF was used as solvent control. The antibacterial activity of the synthesized compounds was found to be mild to moderate antibacterial activity. The synthesized compounds (I–II) were subjected to molecular docking studies of the Glucosamine 6‐Phosphate Synthase. The in silico molecular docking study results showed that, the synthesized compounds may be consider as good inhibitors of GlcN‐6. Also results showed similarity with in vitro tests against bacteria.
In this study the antibacterial efficiency of ethanol extract from Salvia officinalis (L.) growing wild in Kosovo were examined. Ethanol extract was tested against two gram positive bacteria Staphylococus aureus (clinical isolate), Listeria monocytogenes (clinical isolate) and one gram negative bacteria Escherichia coli (clinical isolate). The antibacterial activity was determined by using agar disc diffusion method. The inhibition zone of extract was compared to that of penicillin G. The ethanol extract showed activity in all of the concentrations 1, 3 and 5 mg/mL towards E. coli, S. aureus and L. Monocytogenes. Ethanol extract of the plant with concentration 5 mg/mL showed a stronger antibacterial activity towards bacteria S. aureus with inhibition zone of 9 mm. The antibacterial activity of the S. officinalis (L.)was due to the presence of various secondary metabolites such as phenols and flavonoids. Hence, this plant can be used to discover bioactive natural products that may serve as leads in the development of new pharmaceuticals.
9H-[1,2,4]Triazolo[4,3-g]purin-5-amine (2) was synthesized by reaction of 6-hydrazinyl-7H-purin-2-amine (1a) with formic acid under reflux conditions. Treating compound 1a in ethanol with CS2 in the presence of KOH yielded 5-amino-3H-[1,2,4]triazolo[4,3-g]purine-3-thione (3). The new synthesized compounds were characterized using IR, 1H NMR, and elemental analysis. The synthesized compounds have been screened for antibacterial activity.
The biological activity of heterocyclic compounds depends on their structure, the type of hetero atoms in the ring and on the type of substituents present. In this paper, some heterocyclic compounds with coumarin moieties S1-S5 and novobiocin known as coumarin antibiotic were subjected to the molecular docking studies as important tools for drug discovery. Glucosamine-6-phosphate synthase is selected as a suitable target in this study. In silico studies reveal that all synthesized compounds S1-S5 are good inhibitors of GlcN-6 and the docking results are in agreement with in vitro antibacterial evaluation of compounds S1-S5.
This review describes the preparation of pentacyclic fused heterocycles with the coumarin moiety. These derivatives are reported as biologically active compounds.
10‐chloro‐9h‐5‐oxa‐6b,7,9,11,12‐pentaaza‐benzo[5,6]pentaleno[2,1‐b]naphthalen‐6‐one 2 was synthesized by reaction of 4‐(6‐Chloro‐7H‐purin‐8‐ylamino)‐3‐nitro‐chromen‐2‐one 1 with P(OEt)3 under reflux conditions. Structure of synthesized compound was characterized using IR, NMR spectra and elemental analyses The purified synthesized compound 2 was screened for its antibacterial activity. Compound was screened against Escherichia coli and Bacillus cereus. The antibacterial activity of synthesized compound 2 is compared to antibacterial activity of the standard antibiotics Cephalexine and Streptomycine.
This study presents the synthesis, spectral analysis and antibacterial evaluation of 2‐oxo‐4‐(phenylamino)‐2H‐chromene‐3‐carbaldehyde (3). Compound (3) was synthesized by action of aniline (a) on 4‐chloro‐2‐oxo‐2H‐chromene‐3‐carbaldehyde (2). The synthesized compound was screened for in vitro test of its antibacterial activity against three bacterial cultures: Hafnia alvei, Pseudomonas aeruginosa and Enterobacter cloacae. The antibacterial activity of synthesized compound was compared to antibacterial activity of novobiocin as standard drug. The biological evaluation of compound (3) generally showed moderate activity against Hafnia alvei, Pseudomonas aeruginosa and Enterobacter cloacae compared with novobiocin.
Nucleophilic substitution of 4-chloro-3-nitro-2-oxo-2H-chromen-2-one 3 by 6-chloro-7H-purin-2-ylamine (a), yielded the corresponding 4-(6-chloro-7H-purin-8-ylamino)-3-nitro-chromen-2-one 4. The chemical structure of synthesized compound was characterized using IR and NMR spectra, and elemental analyses. The purified synthesized compound 4 was tested at concentrations 1, 3, 5mg/ml for its antibacterial activity against three bacterial cultures: Staphylococcus aureus, Escherichia coli, and Bacillus cereus. The antibacterial activity of synthesized compound was compared to antibacterial activity of standard antibiotics cephalexine and streptomycin.
4-(5-(Methylthio)-1,3,4-thiadiazol-2-ylamino)-2-oxo-2H-chromene-3-carbaldehyde (3) and 4-(5-(ethylthio)-1,3,4-thiadiazol-2-ylamino)-2-oxo-2H-chromene-3-carbaldehyde (4) were prepared. The structures of the newly synthesized compounds were characterized by infrared (IR), nuclear magnetic resonance (NMR) spectral data and elemental analysis. The synthesized compounds were screened in vitro for their antibacterial activities. The synthesized compounds demonstrated moderate antimicrobial activity.