Relevant bibliographies by topics / Antimicrobial activity of cinnoline derivatives

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  2. Dissertations / Theses
  3. Books
  4. Book chapters
  5. Conference papers

Academic literature on the topic 'Antimicrobial activity of cinnoline derivatives'

Author: Grafiati
Published: 5 June 2025
Last updated: 8 July 2025

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Journal articles on the topic "Antimicrobial activity of cinnoline derivatives"

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Gautam, Nidhi, and O. P. Chourasia. "ChemInform Abstract: Synthesis, Antimicrobial and Insecticidal Activity of Some New Cinnoline Based Chalcones and Cinnoline Based Pyrazoline Derivatives." ChemInform 41, no. 44 (2010): no. http://dx.doi.org/10.1002/chin.201044161.

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ABBADY, M. S., SH M. RADWAN, and E. A. BAKHITE. "ChemInform Abstract: Synthesis and Antimicrobial Activity of Some Cinnoline Derivatives Containing Sulfonamido Group." ChemInform 25, no. 18 (2010): no. http://dx.doi.org/10.1002/chin.199418158.

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R., GOPIKUMAR MENON, and PURUSHOTHAMAN E. "Synthesis of Biologically Active 5-( 4-Hydroxycinnolin-3-yl)tetrazoles and 2-Methyl-5-( 4-acetoxycinnolin-3-yl)-1 ,3,4-oxadiazoles." Journal of Indian Chemical Society Vol. 74, Feb 1997 (1997): 123–24. https://doi.org/10.5281/zenodo.5875232.

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Department of Chemistry, University of Calicut, Calicut-673 635 <em>Manuscript received 29 November 1994, revised 5 July 1995. accepted 14 August 1995</em> A series of 5-(4-hydroxycinnolin-3-yl)tetrazoles and 2-methyl-5-(4-acetoxycinnolin-3-yl)-1,3.4-oxadiazo)es have been synthesised. The compounds exhibited moderate antimicrobial activity. None of the tetrazoles showed any antihistaminic activity.
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M., R. Patel, D. Akbari J., H. Purohit D., and S. Joshi H. "Synthesis and evaluation of pharmacological activity of some new aminopyrimidine and thiopyrimidine derivatives." Journal of Indian Chemical Society Vol. 84, Nov 2007 (2007): 1169–73. https://doi.org/10.5281/zenodo.5824805.

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Department of Chemistry, Saurashtra University, Rajkot-360 005, Gujarat, India <em>E-mail </em>: drhsjoshi@yahoo.com <em>Manuscript received 15 January 2007, revised 6 June 2007, accepted 17 August 2007</em> Various 3-(2-amino-6-arylpyrimidin-4-yl)-6-chlorocinnolin-4(3<em>H)</em>-one (2a-j) and 6-chloro-3-(6-aryl-2-mercapto3,4-dihydropyrimidin-4-yl)cinnolin-4(3<em>H</em>)-one (3a-j) were synthesized by the reaction of 6-chloro-3-[(2<em>E</em>)-3-arylprop-2-enoyl]- cinnolin-4(3<em>H</em>)-ones (1a-j) with guanidine hydrochloride and thiourea respectively. All newly synthesized compounds were tested against different microbes for their antimicrobial activity and <em>Mycobacterium tuberculosis</em> for their antitubercular&nbsp;activity.
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Lewgowd, Wieslawa, and Andrzej Stanczak. "Cinnoline Derivatives with Biological Activity." Archiv der Pharmazie 340, no. 2 (2007): 65–80. http://dx.doi.org/10.1002/ardp.200500194.

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Dr. M.Rajasekaran, Dr M. Rajasekaran, H. B. Nihal Furkhan H.B.Nihal Furkhan, R. Nishanth R.Nishanth, N. Panneerselvam N.Panneerselvam, B. S. Nithishkumar B.S.Nithishkumar, and M. Pandiyan M.Pandiyan. "Synthesis and Docking Studies of Cinnoline Derivatives for Enhanced Anti-Bacterial Activity." International Journal of Pharmaceutical Research and Applications 10, no. 2 (2025): 1797–815. https://doi.org/10.35629/4494-100217971815.

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This study involves the synthesis and evaluation of a series of cinnoline derivatives for their biological activities. The compounds were synthesized through a multi-step process, including the preparation of benzene diazonium chloride, formation of phenyl hydrazoneacetylacetone, synthesis of 4-methyl-3-acetyl cinnoline, and subsequent reactions with various amines. These compounds were characterized using Thin Layer Chromatography (TLC), melting point determination, solubility tests, and advanced spectroscopic techniques, including Infrared (IR) and Proton Nuclear Magnetic Resonance (1HNMR) spectroscopy, to confirm their structures.The compounds demonstrated good solubility in common solvents, and their yields varied depending on the reaction steps. Antibacterial testing was conducted using the cup plate method against Staphylococcus aureus and Escherichia coli, revealing moderate to promising antibacterial activity, with Compound G showing superior activity compared to others, particularly Compound A.In addition, docking studies indicated that some of these cinnoline derivatives exhibited favorable binding energies, especially in comparison to the standard antibiotic Ciprofloxacin, against targets such as dihydrofolatereductase and DNA gyrase. These findings suggest that cinnoline derivatives hold potential as antibacterial agents. Further optimization and pharmacological evaluation are recommended for these compounds.
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Szumilak, Marta. "Polyamine derivatives as potential bisintercalators with antiproliferative activity." Postępy Polskiej Medycyny i Farmacji 4 (June 24, 2016): 9–15. http://dx.doi.org/10.5604/01.3001.0011.6389.

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Bisntercalators are very interesting group of compounds with potential antitumor activity. They interact reversibly with DNA double helix. These agents share common structural features such as the presence of two, planar, polycyclic aromatic or heteroaromatic systems separated by a spacer chain which must be long enough to enable double intercalation between base pairs. The unique chemical structure of these compounds provides numerous modifications within their structure resulting either in higher activity or increased selectivity toward tumor cells. Within the framework of the project, new polyamine derivatives containing dimeric phthalimide, quinoline, cinnoline and chromone moieties were obtained. Three different polyamines: 1,4-bis(3-aminopropyl)piperazine, 4,9-dioxa-1,12-dodecanediamine, 3,3’-diamino-N-methyldipropylamine were used as linkers. The biological activity of compounds was assessed in vitro in a highly aggressive melanoma cell line A375. Quinoline derivatives were found to have a higher antiproliferative activity than cinnoline ones. The lowest IC50 values, below 20 μM, were obtained for quinoline and 2H-chromene-2,4(3H)-dione derivatives. Quinoline diamides were more efficient than cinnoline ones. Polyamine diimides containing phthalimide moieties demonstrated no inhibitory activities against melanoma cells. Preliminary studies of mechanism of action have shown that obtained derivatives were capable of quenching the fluorescence of ethidium bromide-DNA complex, indicating that they bound to ds-DNA in competition with ethidium bromide for binding sites. All the compounds were also subjected to preliminary in silico ADME screening by evaluating their theoretical drug-likeness and physicochemical properties using Discovery Studio 3.0 obtained from Accelrys. Compounds meeting the required ADME and drug-likeness criteria were selected.
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Prashanthi Evangeline M, Prem Kumar P, and Bala Murugan K. "Cinnoline Derivatives as Antibacterial Agent and Antimycobacterial Agent: Synthesis, Microbial Evaluation and Molecular Docking Study." International Journal of Research in Pharmaceutical Sciences 11, no. 4 (2020): 6675–84. http://dx.doi.org/10.26452/ijrps.v11i4.3588.

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Fourteen Novel cinnoline library compounds were designed, synthesized through a facile approach, and allowed for screening for anti-bacterial activity and anti-tubercular activity. The titled compounds were entirely synthesized by replacing alkyl groups, sulphonyl, halo groups in the 6th &amp; 7th position of cinnoline moiety. The enlightenment of structure was done by FTIR HNMR along with elemental analysis and further docked for Structural activity. The newly synthesized Cinnoline Compounds were examined for their in vitro drug-sensitive M tuberculosis H37Hv strain. All the compounds have shown MIC between &gt;100-12.5 μg /ml. In this investigation, we Evaluated all the compounds for Anti-bacterial activity. The main compounds were initially tested in vitro for Anti-bacterial activity against gram-positive and gram-negative bacteria by using the Disk plate method. The most active Compound 10 exhibited 12.5 μg /ml inhibitions against drug-sensitive M Tuberculosis H37Rv strain. Among all synthesized compounds CN-7 was found to be a Hit compound with MIC value 12.5 ug/ml Against E Coli.
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Lettreuch, H., M. Khodja, and H. Boutoumi. "New Synthetic Route to Cinnoline Derivatives and Their Microbiological Activity." Russian Journal of Organic Chemistry 56, no. 12 (2020): 2188–93. http://dx.doi.org/10.1134/s1070428020120222.

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Kandeel, Manal M., Aliaa M. Kamal, Bassem H. Naguib, and Marwa S. A. Hassan. "Design, Synthesis, Cytotoxic Activity and Apoptosis-inducing Action of Novel Cinnoline Derivatives as Anticancer Agents." Anti-Cancer Agents in Medicinal Chemistry 18, no. 8 (2018): 1208–17. http://dx.doi.org/10.2174/1871520618666180220121319.

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Aims: Tyrosine kinases and topoisomerase I are common target enzymes for the majority of the anticancer agents. In contrast to quinazolines and quinolines, kinase inhibitors and topoisomerase inhibitors incorporating cinnoline scaffold are relatively infrequent. Thus the aim of this work was to replace the former scaffolds with the latter one. Eighteen novel cinnoline derivatives were designed, synthesized and characterized using both microanalytical and spectral data. Methods: The cytotoxic activity of the new compounds was screened in vitro against both human breast cancer cells and normal breast cells. Results: The enzymatic inhibition activity of promising candidates against both epidermal growth factor receptor tyrosine kinase and topoisomerase I was accomplished. Conclusions: Cell cycle profiles were observed at IC50 doses of representative biologically active compounds. Compound 7 represented a new scaffold incorporating triazepinocinnoline ring system and showed outstanding cytotoxic activity against MCF-7 (0.049 µM), tyrosine kinase inhibition (0.22 µM), apoptosis percentage and the highest selectivity index.
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Dissertations / Theses on the topic "Antimicrobial activity of cinnoline derivatives"

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Nascimento, PatrÃcia Georgina Garcia do. "Obtaining of derivatives lithocholic acid and antimicrobial activity." Universidade Federal do CearÃ, 2012. http://www.teses.ufc.br/tde_busca/arquivo.php?codArquivo=16720.

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CoordenaÃÃo de AperfeÃoamento de Pessoal de NÃvel Superior<br>This paper describes obtaining eight lithocholic acid derivatives, as well as inhibitory activity. Interest in the use of lithocholic acid as starting material for the preparation of derivatives arose because of it being widely studied in order to discover new biological activities and such studies have shown good results. In this work it was used for the synthesis of a series of derivatives with modifications at the C-3 and/or C-24 of the steroid skeleton. The series was prepared using simple chemical and showed good yields. Aiming to investigate the antibacterial activity of the same and its derivatives, aiming to structure-activity relationships, tests were performed with bacteria Escherichia coli, Staphylococcus aureus, Bacillus cereus and Pseudomonas aeruginosa, try some of them presented significant results. And lithocholic acid derivatives were characterized by spectroscopic IR, 1H NMR, 13C-BB NMR and 13C-DEPT NMR and mass spectrometry as well as comparison with data in the literature and described constitute the body of the dissertation.<br>Esse trabalho descreve a obtenÃÃo de oito derivados do Ãcido litocÃlico, bem como, suas atividades antimicrobianas. O interesse pela utilizaÃÃo do Ãcido litocÃlico como material de partida na preparaÃÃo de derivados surgiu pelo fato do mesmo sendo bastante estudado com o objetivo de descobrir novas atividades biolÃgicas e tais estudos terem apresentado bons resultados. Nesse trabalho, o Ãcido litocÃlico foi submetido a modificaÃÃes moleculares nas posiÃÃes C-3 e/ou C-24 do esqueleto esteroidal. A sÃrie foi preparada utilizando quÃmica convencional e apresentando bons rendimentos. Com o objetivo de investigar a atividade antimicrobiana dos compostos, foram realizados testes com as bactÃrias Escherichia coli, Staphylococcus aureus, Bacillus cereus e Pseudomonas aeruginosa, tento alguns deles apresentado resultados bastante significativos. O Ãcido litocÃlico e seus derivados foram caracterizados por mÃtodos espectroscÃpicos de IV, RMN 1H, RMN 13C-BB e RMN 13C-DEPT e por espectrometria de massa, bem como comparaÃÃo com dados descritos na literatura.
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Chakraborty, Madhumita. "Studies on the antimicrobial activity of available triterpenoids and its derivatives from some medicinal plants." Thesis, University of North Bengal, 2012. http://hdl.handle.net/123456789/1443.

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Alasmary, Fatmah A. S. "Synthesis and evaluation of selected benzimidazole derivatives as potential antimicrobial agents. An investigation into the synthesis of substituted benzimidazoles and their evaluation in vitro for antimicrobial activity." Thesis, University of Bradford, 2013. http://hdl.handle.net/10454/6325.

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Microbe resistence is a serious issue, especially as they have become resistant to most well known drugs. Therefore this is considered as a global problem and is now dealt with at a poitical level. Since no new classes of antimicrobial agents have been discovered in the past three deacdes, the development of new drugs is extremely urgent. Therefore the aim of this project was to synthesise derivatives of benzimidazole, and then assesses their antimicrobial activities in vitro by using disc (well) diffusion and MICs tests. A total of 69 benzimidazole derivatives, with substituents at positions 1, 2, and 5, were synthesised, characterised and tested against selected bacteria and fungi. In addition, six bezimidazole silver complexes were prepared and evaluated for their antimicrobial behavior. The SAR showed that the antimicrobial activity of the compounds depended on the substituents attached to the bicyclic heterocycle. Some promising results were obtained. In particular, 5 compounds displayed antibacterial activity against two MRSA strains with MIC values corresponding to ciprofloxacin, which can be considered significant. The compounds have some common features; four possess 5-chloro or 5-bromo substituents; two are derivatives of (S)-2- ethanaminebenzimidazole and the others are derivative of one 2-(chloromethyl)-1Hbenzo[d]imidazole, (1H-benzo[d]imidazol-2-yl)methanethiol and 2-(methoxymethyl)-1-methyl-1H-benzo[d]imidazole. The results from the antifungal screening were very interesting as there were 26 compounds, including two silver complexes, which were potent fungicides against the selected fungal species. They showed equivalent or greater potentency in their MIC values than amphotericin B. In particular, the 5-fluoro, 5-chloro and 5-bromo benzimidazole showed broad spectrum activity.<br>Saudi Culture Bureau and King Saud University
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Alasmary, Fatmah Ali Saeed. "Synthesis and evaluation of selected benzimidazole derivatives as potential antimicrobial agents : an investigation into the synthesis of substituted benzimidazoles and their evaluation in vitro for antimicrobial activity." Thesis, University of Bradford, 2013. http://hdl.handle.net/10454/6325.

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Microbe resistence is a serious issue, especially as they have become resistant to most well known drugs. Therefore this is considered as a global problem and is now dealt with at a poitical level. Since no new classes of antimicrobial agents have been discovered in the past three deacdes, the development of new drugs is extremely urgent. Therefore the aim of this project was to synthesise derivatives of benzimidazole, and then assesses their antimicrobial activities in vitro by using disc (well) diffusion and MICs tests. A total of 69 benzimidazole derivatives, with substituents at positions 1, 2, and 5, were synthesised, characterised and tested against selected bacteria and fungi. In addition, six bezimidazole silver complexes were prepared and evaluated for their antimicrobial behavior. The SAR showed that the antimicrobial activity of the compounds depended on the substituents attached to the bicyclic heterocycle. Some promising results were obtained. In particular, 5 compounds displayed antibacterial activity against two MRSA strains with MIC values corresponding to ciprofloxacin, which can be considered significant. The compounds have some common features; four possess 5-chloro or 5-bromo substituents; two are derivatives of (S)-2- ethanaminebenzimidazole and the others are derivative of one 2-(chloromethyl)-1Hbenzo[d]imidazole, (1H-benzo[d]imidazol-2-yl)methanethiol and 2-(methoxymethyl)-1-methyl-1H-benzo[d]imidazole. The results from the antifungal screening were very interesting as there were 26 compounds, including two silver complexes, which were potent fungicides against the selected fungal species. They showed equivalent or greater potentency in their MIC values than amphotericin B. In particular, the 5-fluoro, 5-chloro and 5-bromo benzimidazole showed broad spectrum activity.
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Sobola, Abdullahi Owolabi. "Synthesis, characterization and antimicrobial activity of copper (II) complexes of some hydroxybenzaldimines and their derivatives." Thesis, Rhodes University, 2012. http://hdl.handle.net/10962/d1016258.

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This study focuses on the antimicrobial activity of Cu(II) complexes of some orthohydroxybenzaldimines and its derivatives. Four different categories of Schiff base ligands were prepared by condensing salicylaldehyde, o-vanillin, p-vanillin and vanillin with p- and osubstituted anilines; 1-aminonaphthalene; 2- and 3-aminopyridine; 2- and 3- aminomethylpyridine as well as 2-aminobenzimidazole. The last category was prepared from ophenylenediamine and o-vanillin. The Schiff base ligands have been characterized by a combination of elemental analysis and spectral (¹H- and ¹³C-NMR, UV/Visible, infrared and Raman) data. The existence of strong intramolecular hydrogen bonding in the orthohydoxybenzaldimines was evident from the chemical shift values of the hydroxyl proton in the ¹H-NMR spectra of the Schiff base ligands. The hydroxyl proton resonates at high frequency and thus absorbed far downfield at 13.46-11.83 ppm, reflecting the presence of hydrogen bonding between the hydroxyl proton and the imine nitrogen. In the p-substituted aniline analogues of the Schiff base, a plot of the chemical shift values of the hydroxyl proton against the Hammett's substituent parameters gave a linear correlation between the electronegativities of the substituents and the chemical shift values. The nitro group with the highest electronegativity caused the least deshielding of the hydroxyl proton and thus absorbed upfield compared to the less electronegative substituents such as the CH3 and OCH3 analogues. Likewise, in the solid state infrared spectra of the ligands, the hydroxyl stretching band of the ortho-hydroxyl Schiff base ligands was observed as a very broad band and at much lower frequency, 3100-2100 cm⁻¹, indicating the existence of strong intramolecular hydrogen bonding. In the same vein, ¹H- and ¹³C-NMR spectral data for the Schiff base ligands indicated that the prepared compounds exist in the enol form in aprotic solvent, chloroform. The methine proton appeared as singlet and there was no carbonyl signal in the ¹³C-NMR spectra of the Schiff base ligands. This was supported by the infrared data having no vibrational band attributable to the carbonyl stretching of the keto-form of the Schiff base ligands in solid state. However, the UV/Visible study of the Schiff base ligands in protic solvent, methanol, suggested the existence of some of the Schiff base ligands in keto-enol form. A band at greater than 400 nm was observed in the UV/Visible spectra of the ligands and this has been attributed to the presence of the keto form of orthohydroxyl Schiff base ligands in solution. A plot of the molar absorptivity (ε) of the band at greater than 400 nm against Hammett substituent parameters revealed that the intensity of the bands increased with the electronegativity of the substituents. The Cu(II) complexes of salicylaldehyde, o-vanillin and a few p-vanillin based Schiff base ligands are reported in this work. It was observed that introduction of Cu(II) ions into the ligand system resulted in the hydrolysis of the imine band in few cases. All the isolated complexes have been characterized by elemental analysis, conductivity measurement, infrared and UV/Visible spectral data. The structures of three of the Cu(II) complexes were further confirmed by X-ray single crystal diffraction. The Schiff base ligands either coordinated as neutral base through the imine nitrogen or via the imine nitrogen and the phenolic oxygen atoms. In addition, the benzimidazole-based and ovan-2-pico analogues equally coordinated through the imidazole N-3 nitrogen and the azine nitrogen respectively; thus acted as tridentate. In general, the synthesized Cu(II) complexes fell into seven categories viz: [Cu(LH)Cl(H₂O)]Cl; [Cu(LH)₂Cl₂].xH₂O; [CuL₂]; [Cu₂L₂]; [Cu(LH)Cl(H₂O)]Cl; and [MLCl]. The Cu(II) complexes of the form, M(LH)₂Cl₂.xH₂O were either 1:1 or non-electrolyte in methanol and DMF. The third category, CuL₂, was however, non-electrolyte existing as neutral four coordinate Cu(II) complexes. X-ray single crystal structure of Cu(II) complexes derived from the ammonia-based Schiff bases revealed a square planar geometry for the complexes and this agreed with the planar geometry that has been reported for Cu(II) complexes of N-arylsalicylaldimines of the type studied in this work. The complexes, [Cu₂L₂], resulted from the ortho-hydroxyaniline analogues and were polymeric with the Schiff base ligands coordinating to the Cu(II) ions as tridentate dibasic via the imine nitrogen, phenolic oxygen and the aminophenolic oxygen atoms. Cu(II) complexes prepared from ovan-2-ampy and ovan-2-pico Schiff bases were of the forms [Cu(LH)Cl(H₂O)]Cl and [CuLCl] respectively. The X-ray crystal structure of [Cu(ovan-2- pico)Cl] revealed a four-coordinate square planar geometry for the complex. In the same vein, the o-phenylenediamine complexes were of the form [Cu(L)(H₂O)], with the X-ray crystal structure of [Cu(bis-ovanphen)(H₂O)] revealing a square pyramidal geometry. The Schiff base ligands and the isolated Cu(II) complexes have been evaluated for their antimicrobial activity against three bacterial strains (Escherichia coli ATCC® 8739™*, Staphylococcus aureus subsp. aureus ATCC® 6538™* and Bacillus subtilis subsp. spizizeni ATCC® 6633™*) and one fungal strain, Candida albicans ATCC® 2091™*, using agar disc diffusion and broth dilution techniques. It was observed that the presence of the methoxyl group at the ortho-position of the aldehyde moiety of the Schiff base ligands enhanced the activity of the ligand tremendously and thus the o-vanillin analogues showed the highest potency against the tested organisms. In addition, the hydroxyaniline analogues were equally the most promising of all the substituted aniline based Schiff bases. The o-vanillin analogues of the aminopyridines and aminomethylpyridines also exhibited significant activity against the tested organisms. All the 2-aminobenzimidazole series were active against the tested organisms. It should be noted that E. coli was the least susceptible of all the microorganisms while the highest potency was exhibited against the fungus of choice, Candida albicans. Lastly, chelation of the Schiff base ligands with Cu(II) ions did not have significant influence on the activity of the free ligands.
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Gaivelytė, Kristina. "5-nitrofuraldehido darinių antimikrobinio aktyvumo tyrimas, toksiškumo, farmakokinetikos ir struktūros aktyvumo ryšio įvertinimas." Master's thesis, Lithuanian Academic Libraries Network (LABT), 2010. http://vddb.laba.lt/obj/LT-eLABa-0001:E.02~2010~D_20100621_093138-22354.

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5-nitrofuraldehido darinių antimikrobinio aktyvumo tyrimas, toksiškumo, farmakokinetinių savybių ir struktūros aktyvumo ryšio įvertinimas. K. Gaivelytės magistro baigiamasis darbas. Moksliniai vadovai: dr. V. Petrikaitė, dr. J. Šarlauskas, prof. habil. dr. A. Pavilonis; Kauno medicinos universiteto, Farmacijos fakulteto, Vaistų chemijos katedra. Kaunas, 2010. Darbo tikslas – įvertinti 5-nitrofuraldehido darinių struktūros įtaką jų antimikrobiniam aktyvumui ir parinkti perspektyviausius antimikrobinius junginius tolimesniems tyrimams. Tyrimo metodai. Junginių antimikrobinio aktyvumo prognozė atlikta panaudojant PASS programą. Antimikrobinis aktyvumas ištirtas in vitro serijinio skiedimo standžioje terpėje metodu. Junginių farmakokinetinių savybių ir toksiškumo prognozė atlikta, panaudojant ADME/Tox Boxes programą. Tyrimo rezultatai. PASS programa antibakterinį ir priešgrybelinį aktyvumą prognozavo visiems tiriamiems junginiams. Atlikus tyrimus in vitro, nustatyta, kad junginių aktyvumas prieš įvairius mikroorganizmus skyrėsi, nitrofurano fragmento neturintys junginiai buvo visai neaktyvūs. Nitrofurano bisdariniai yra gana aktyvūs prieš visas bakterijas (MSK = 0,5 100 μg/ml), išskyrus P. aeruginosa, K. pneumoniae ir P. mirabilis. Bisjunginys BIC-34, turintis butilo fragmentą, buvo aktyviausias prieš S. aureus, E. faecalis ir B. subtilis, o piridino liekaną turintis bisjunginys BIC 67 – prieš K. pneumoniae, P. aeruginosa, P. mirabilis (MSK = 50 μg/ml). Gali būti, kad šio... [toliau žr. visą tekstą]<br>Analysis of 5-nitrofuraldehyde derivatives antimicrobial activity, evaluation of toxicity, pharmacokinetic properties and structure – activity relationship. K. Gaivelytė Master Thesis. Scientific supervisors: Dr. V. Petrikaitė, Dr. J. Šarlauskas, Prof. Habil. Dr. A. Pavilonis; Kaunas University of Medicine, Faculty of Pharmacy, Department of Medicinal Chemistry. Kaunas, 2010. The Aim of the Research – to evaluate the influence of the structure of 5-nitrofuraldehyde derivatives and identify the most promising compounds for the further research. Methods. Prognosis of antimicrobial activity of all compounds was carried out by using PASS software. Antimicrobial activity was tested in vitro by using a serial dilution in agar technique. Pharmacokinetic properties and toxicity were predicted by using ADME/Tox Boxes program. Results. PASS program predicted antibacterial and antifungal activity for all tested compounds. The results of experiments in vitro showed that activity against various microorganisms was different; compounds without nitrofuran fragment were not active. Biscompouds were active enough against all bacteria (MIC = 0,5-100 μg/ml), except P. aeruginosa, K. pneumoniae and P. mirabilis. Biscompoud possessing butyl fragment in its structure was the most active against S. aureus, E. faecalis and B. subtilis and biscompound BIC-67 with the moiety of pyridine was the most active against K. pneumoniae, P. aeruginosa, P. mirabilis (MIC = 50 μg/ml). It could be that the... [to full text]
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Srđan, Bjedov. "Sinteza i biološka ispitivanja novih derivata žučnih kiselina." Phd thesis, Univerzitet u Novom Sadu, Prirodno-matematički fakultet u Novom Sadu, 2017. https://www.cris.uns.ac.rs/record.jsf?recordId=104087&source=NDLTD&language=en.

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U disertaciji je ostvarena sineza amida i oksazolina žučnih kiselina, kao i njihovih alkil i alkilidenskih derivata polazeći od holne kiseline. Ipitano je pona&scaron;anje različitih okso derivata žučnih kiselina u uslovima Grignard-ove i Wittig-ove reakcije. Ispitana je biolo&scaron;ka aktivnost odabranih sintetizovanih jedinjenja<br>Synhesis of bile acid amide and oxazoline derivatives, and their alkyl and alkylidene derivatives was accomplished starting from cholic acid. Also, chemical behavior of different bile acid oxo derivatives in Grignard and Wittig reaction was investigated. Biological activity&nbsp; of selected synthesized compounds was evaluated.
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Milica, Karadžić. "Хроматографска, микробиолошка и in silico анализа стероидних једињења од потенцијалног биомедицинског значаја". Phd thesis, Univerzitet u Novom Sadu, Tehnološki fakultet Novi Sad, 2017. http://www.cris.uns.ac.rs/record.jsf?recordId=104606&source=NDLTD&language=en.

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Испитивано је хроматографско понашање (хроматографска липофилност) 29 стероидних једињења (триазола и тетразола, толуенсулфонилхидразида, диона, нитрила и динитрила) од потенцијалног биомедицинског значаја, испитивано је помоћу течне хроматографије високих перформанси на обрнутим фазама, применом две стационарне и две мобилне фазе. Липофилност, изражена преко ретенционог параметра logk, моделована је QSRR приступом. Формирани линеарни и нелинеарни модели омогућили су испитивање односа између ретенционих параметара и in silico молекулских дескриптора, који су израчунати на основу структуре испитиваних једињења. Добра предиктивна моћ формираних модела, добијених за калибрациони сет, потврђена је и применом екстерног тест сета и валидационог сета. Предиктивна моћ формираних модела потврђује могућност њиховог коришћења за предвиђање липофилности нових, структурно сличних, једињења. Примењене су и класификационе хемометријске методе (анализа главних компоненти и хијерархијска кластер анализа) како би се уочиле сличности и разлика између једињења. Поред тога, представљена је in vitro анализа антимикробног потенцијала испитиваних стероидних једињења према Staphylococcus aureus, Escherichia coli и Candida albicans. Два једињења, са епоксидном групом у положају 4,5, испољила су бактериостатски ефекат према S. aureus. Такође, приказана је докинг анализа одабраних испитиваних једињења са антипролиферативном активношћу према ћелијама андроген-рецептор негативног канцера простате (AR-нег. PC-3). На основу визуелизације оптималних положаја и анализе постојећих интеракција, идентификовано је једињење са највећим потенцијалом као инхибитор хуманог цитохрома P450 CYP17A1.<br>Ispitivano je hromatografsko ponašanje (hromatografska lipofilnost) 29 steroidnih jedinjenja (triazola i tetrazola, toluensulfonilhidrazida, diona, nitrila i dinitrila) od potencijalnog biomedicinskog značaja, ispitivano je pomoću tečne hromatografije visokih performansi na obrnutim fazama, primenom dve stacionarne i dve mobilne faze. Lipofilnost, izražena preko retencionog parametra logk, modelovana je QSRR pristupom. Formirani linearni i nelinearni modeli omogućili su ispitivanje odnosa između retencionih parametara i in silico molekulskih deskriptora, koji su izračunati na osnovu strukture ispitivanih jedinjenja. Dobra prediktivna moć formiranih modela, dobijenih za kalibracioni set, potvrđena je i primenom eksternog test seta i validacionog seta. Prediktivna moć formiranih modela potvrđuje mogućnost njihovog korišćenja za predviđanje lipofilnosti novih, strukturno sličnih, jedinjenja. Primenjene su i klasifikacione hemometrijske metode (analiza glavnih komponenti i hijerarhijska klaster analiza) kako bi se uočile sličnosti i razlika između jedinjenja. Pored toga, predstavljena je in vitro analiza antimikrobnog potencijala ispitivanih steroidnih jedinjenja prema Staphylococcus aureus, Escherichia coli i Candida albicans. Dva jedinjenja, sa epoksidnom grupom u položaju 4,5, ispoljila su bakteriostatski efekat prema S. aureus. Takođe, prikazana je doking analiza odabranih ispitivanih jedinjenja sa antiproliferativnom aktivnošću prema ćelijama androgen-receptor negativnog kancera prostate (AR-neg. PC-3). Na osnovu vizuelizacije optimalnih položaja i analize postojećih interakcija, identifikovano je jedinjenje sa najvećim potencijalom kao inhibitor humanog citohroma P450 CYP17A1.<br>Chromatographic behavior (chromatographic lipophilicity) of 29 steroid compounds (triazole and tetrazole, toluenesulfonylhydrazide, dione, dinitrile and nitrile) with potential biomedical importance was investigated by reversed-phases high-performance liquid chromatography using two stationary and two mobile phases. The lipophilicity expressed through the retention parameter logk was modeled using QSRR approach. Formed linear and non-linear models enabled the study of the relationship between the retention parameters and in silico molecular descriptors calculated from the structure of the investigated compounds. Good predictive power of the established models obtained for the calibration set was confirmed by the application of an external test set and validation set. The predictive power of the established model confirms the possibility of their use for lipophilicity prediction of new, structurally similar compounds. The classification chemometric methods (principal components analysis and hierarchical cluster analysis) were applied in order to recognize the similarities and differences between the compounds. Тhis dissertation presents the in vitro analysis of the antimicrobial potentials of the investigated steroid compounds against Staphylococcus aureus, Escherichia coli and Candida albicans. Two compounds, with epoxy group in the position 4,5, exhibited bacteriostatic effect against S. aureus. The docking analysis of selected test compounds with antiproliferative activity toward cells of androgen receptor-negative prostate cancer (AR-neg. PC-3) is showed. Based on the optimal position visualization and analysis of existing interactions a compound with the most promising potential as human cytochrome P450 CYP17A1 inhibitor is idetified.
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Alasmary, Fatmah A. S., Anna M. Snelling, M. E. Zain, A. M. Alafeefy, A. S. Awaad, and Nazira Karodia. "Synthesis and Evaluation of Selected Benzimidazole Derivatives as Potential Antimicrobial Agents." 2015. http://hdl.handle.net/10454/9303.

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No<br>A library of 53 benzimidazole derivatives, with substituents at positions 1, 2 and 5, were synthesized and screened against a series of reference strains of bacteria and fungi of medical relevance. The SAR analyses of the most promising results showed that the antimicrobial activity of the compounds depended on the substituents attached to the bicyclic heterocycle. In particular, some compounds displayed antibacterial activity against two methicillin-resistant Staphylococcus aureus (MRSA) strains with minimum inhibitory concentrations (MICs) comparable to the widely-used drug ciprofloxacin. The compounds have some common features; three possess 5-halo substituents; two are derivatives of (S)-2-ethanaminebenzimidazole; and the others are derivatives of one 2-(chloromethyl)-1H-benzo[d]imidazole and (1H-benzo[d]imidazol-2-yl)methanethiol. The results from the antifungal screening were also very interesting: 23 compounds exhibited potent fungicidal activity against the selected fungal strains. They displayed equivalent or greater potency in their MIC values than amphotericin B. The 5-halobenzimidazole derivatives could be considered promising broad-spectrum antimicrobial candidates that deserve further study for potential therapeutic applications.
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Ke, Fang-Ying, and 柯方盈. "Studies on the Syntheses of Pyrazoline､Thiazoline Derivatives and their Antimicrobial､Antioxidative Activity." Thesis, 2003. http://ndltd.ncl.edu.tw/handle/06836031465387714444.

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碩士<br>南台科技大學<br>化學工程系<br>91<br>Many heterocyclic compounds have been known for special physiological activity. Therefore, sydnonyl-substituted pyrazolines, thiazolines and thiazolidines were synthesized in this study. The text is divided into two parts: In the first part, the sydnonyl-substituted pyrazoline derivatives were prepared successfully through the reactions of sydnonyl-substituted α, β-unsaturated ketones and hydrazine hydrate. The new series of sydnonyl-substituted pyrazolines were evaluated for their antimicrobial activity. The results indicated that the antifungal activity of these compounds exhibited more potence then antibacterial activity. In the second part, 3-aryl-4-formylsydnone thiosemicarbazones reacted with cyclic reagents, such as ethyl chloroacetate, ethyl 2-chloroacetoacetate and 2-bromoacetophenone to give heterocyclic substituted sydnones that possess 4-oxo-thiazolidine, thiazoline groups. The synthesized compounds were evaluated for the antioxidant activities. The results indicated that almost all the newly synthesized compounds exhibit significant scavenging effects on DPPH (α,α-diphenyl-β-picrylhydrazyl) free redical. Among these compounds, 4-phenyl-2-[(3-arylsydnon-4-yl-methylene)hydrazono]-2,3-dihydrothiazoles possess the potent radical scavenging activities comparable with that of vitamin E.
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Books on the topic "Antimicrobial activity of cinnoline derivatives"

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Jenssen, Havard. Antimicrobial activity of lactoferrin and lactoferrin derived peptides. Nova Science, 2009.

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Kaur, Ms Rajwant. Synthesis and Antimicrobial Activity of 1,3,4-Oxadiazole Derivatives. Independently Published, 2018.

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Kozłowska, Joanna, and Anna Duda-Madej, eds. Antimicrobial Activity of Different Plant Extracts, Plant-Derived Compounds and Synthetic Derivatives of Natural Compounds on Pathogenic Microorganisms. MDPI, 2024. http://dx.doi.org/10.3390/books978-3-7258-1423-7.

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Book chapters on the topic "Antimicrobial activity of cinnoline derivatives"

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Yalpani, Manssur, Fran Johnson, and Larry E. Robinson. "Antimicrobial Activity of Some Chitosan Derivatives." In Advances in Chitin and Chitosan. Springer Netherlands, 1992. http://dx.doi.org/10.1007/978-94-011-5942-5_61.

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Feio, S. S., A. M. Silva, L. Reis, B. Gigante, J. C. Roseiro, and M. J. Marcelo-Curto. "Antimicrobial Activity of Dehydroabietic Acid Derivatives (II)." In Natural Products in the New Millennium: Prospects and Industrial Application. Springer Netherlands, 2002. http://dx.doi.org/10.1007/978-94-015-9876-7_25.

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van Doorne, H., E. H. Bosch, and C. F. Lerk. "Interactions between Cyclodextrins and Some Antimycotic Imidazole Derivatives: Studies on Solubility and Antimicrobial Activity." In Proceedings of the Fourth International Symposium on Cyclodextrins. Springer Netherlands, 1988. http://dx.doi.org/10.1007/978-94-009-2637-0_42.

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Hoogkamp-Korstanje, J. A. A. "Comparative in Vitro Activity of Five Quinoline Derivatives and Five Other Antimicrobial Agents Used in Oral Therapy." In Ciprofloxacin. Vieweg+Teubner Verlag, 1986. http://dx.doi.org/10.1007/978-3-663-01930-5_2.

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Filipowska, Anna, Wojciech Filipowski, Ewaryst Tkacz, and Monika Wujec. "Statistical Analysis of the Impact of Molecular Descriptors on Antimicrobial Activity of Thiourea Derivatives Incorporating 3-amino-1,2,4-triazole Scaffold." In Innovations in Biomedical Engineering. Springer International Publishing, 2017. http://dx.doi.org/10.1007/978-3-319-70063-2_19.

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Ambhore, Ajay N. "An Efficient Green Synthesis of Diphenyl Pyrazol-4-Yl-Thiopyridin-4-Yl-1,3,4-Oxadiazole Derivatives and Evaluation of Their Antimicrobial and Antioxidant Activity." In Modern Green Chemistry and Heterocyclic Compounds. Apple Academic Press, 2020. http://dx.doi.org/10.1201/9780367276942-3.

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Penta, Santhosh. "Antimicrobial Agents." In Advances in Structure and Activity Relationship of Coumarin Derivatives. Elsevier, 2016. http://dx.doi.org/10.1016/b978-0-12-803797-3.00002-3.

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Dutta, Joydeep, and Pradip Dutta. "Antimicrobial Activity of Chitin, Chitosan and Their Oligosaccharides." In Chitin, Chitosan, Oligosaccharides and Their Derivatives. CRC Press, 2010. http://dx.doi.org/10.1201/ebk1439816035-c15.

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Durgadevi, Ravindran, and Arumugam Veera Ravi. "Synthetic Derivatives from Marine Natural Products as Potential Antimicrobial Drugs." In Frontiers in Antimicrobial Agents. BENTHAM SCIENCE PUBLISHERS, 2023. http://dx.doi.org/10.2174/9789815080148123030016.

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The marine environment havens a massive number of species that are the source of a wide range of structurally diverse bioactive secondary metabolites. The importance of marine natural products (MNPs) in drug discovery has been documented extensively with their impact on the development of existing drugs. Despite the promising activity of MNPs, most of them suffer from their complex structures, instability, and poor solubility. The synthetic derivatives of natural products cover the chemical derivatization of scaffolds isolated from marine sources and are highly applicable as chemical biosynthesis and structural modifications provide new insights into the bioactivities and the dealings against specific targets that are important for exploring the indefinite chemical space. Also, engineering of the biosynthetic pathway has shown its ability to drive analogies arising from a variety of alterations, including replacement of residues, feeding with non-natural precursors, and enzyme knockout. Such arrays of synthetic compounds execute functionally distinct biological activities against various microbial pathogens, considering MNPs valuable products in the current era of drug discovery. This chapter describes the strategies and principles for the development of synthetic drugs, as divulged by several fruitful medicines that are derived from marine origin.&lt;br&gt;
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Pal, Pinki. "Recent advances in syntheses and antibacterial activity of novel furan derivatives." In Heterocyclic Chemistry - New Perspectives [Working Title]. IntechOpen, 2024. http://dx.doi.org/10.5772/intechopen.1004117.

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Microbial resistance has turned into a global issue due to the ineffectiveness of currently available antimicrobial medicines. In the realm of medicinal chemistry, furan derivatives have taken on a special position. An essential synthetic technique in the search for new drugs is the inclusion of the furan nucleus. Due to the remarkable therapeutic efficacy of furan-related medicines, medicinal chemists have been inspired to create numerous innovative antibacterial agents. Due to the numerous methods by which furans derivatives can be made as well as their numerous structural reactions, the field of organic chemistry and medicinal chemistry offers a wide range of prospects. To combat the enduring issue of microbial resistance, the crucial facts presented in this chapter may aid in the creation of more effective and secure antimicrobial agents.
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Conference papers on the topic "Antimicrobial activity of cinnoline derivatives"

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Al-Majedy, Yasmien, Ahmed Al-Amiery, and Redha Al-Bayati. "Novel quinazolinone derivatives: Synthesis and Antimicrobial Activity." In The 14th International Electronic Conference on Synthetic Organic Chemistry. MDPI, 2010. http://dx.doi.org/10.3390/ecsoc-14-00413.

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Mangalagiu, Violeta, Dorina Amariucai-Mantu, Vasilichia Antoci, Dumitrela Diaconu, and Ionel I. Mangalagiu. "Azine derivatives with antimicrobial properties." In Conferința științifică națională cu participare internațională "Integrare prin cercetare și inovare", dedicată Zilei Internaționale a Științei pentru Pace și Dezvoltare. Moldova State University, 2025. https://doi.org/10.59295/spd2024n.87.

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Azine derivatives, especially pyridine, quinoline and their fused derivatives, are invaluable scaffolds in medicinal chemistry having a large variety of biological activities, antimicrobials including. In this work we present some recent results that we obtained in the field of azine with antibacterial, antifungal and antituberculosis activity. Some of the obtained results are very promising, the antimicrobial activity of some azine derivatives being spectacular.
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Smit, Biljana, Ivana Radojevic, Marijana Djukic, Ljiljana Comic, and Darko Asanin. "Antimicrobial Activity of Various Hydantoin Derivatives ." In 2nd International Electronic Conference on Medicinal Chemistry. MDPI, 2016. http://dx.doi.org/10.3390/ecmc-2-a032.

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Babu, Kayathi Narendra, Tamatam Rekha, G. Sravya, Putta Ramachandra Reddy, Venkatapuram Padmavathi, and Grigory V. Zyryanov. "Synthesis and antimicrobial activity of bis(azolyl) urea derivatives." In PROCEEDINGS OF THE 3RD INTERNATIONAL CONFERENCE ON AUTOMOTIVE INNOVATION GREEN ENERGY VEHICLE: AIGEV 2018. Author(s), 2019. http://dx.doi.org/10.1063/1.5087354.

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Lysytsya, Andriy, and Pavlо Kryvoshyya. "COMPARISON OF ANTIMICROBIAL ACTIVITY OF TWO POLYMERIC GUANIDINE DERIVATIVES." In GRUNDLAGEN DER MODERNEN WISSENSCHAFTLICHEN FORSCHUNG. European Scientific Platform, 2023. http://dx.doi.org/10.36074/logos-31.03.2023.23.

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Fulgheci, Ana Maria, Ioana Nicolau, Petre Ionita, et al. "STUDY OF THE ANTIMICROBIAL ACTIVITY OF SOME FERROCENE DERIVATIVES." In International Symposium "The Environment and the Industry". National Research and Development institute for Industrial Ecology, 2022. http://dx.doi.org/10.21698/simi.2022.ab16.

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Negreanu-Pirjol, Ticuta. "ANTIMICROBIAL ACTIVITY OF SOME TRANSITIONAL METAL COMPLEXES WITH PHENYLBIGUANIDE DERIVATIVES." In 15th International Multidisciplinary Scientific GeoConference SGEM2015. Stef92 Technology, 2015. http://dx.doi.org/10.5593/sgem2015/b61/s25.036.

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Sankar, P. Siva, K. Divya, G. Dinneswara Reddy, V. Padmavathi, and Grigory V. Zyryanov. "Synthesis, characterization and antimicrobial activity of azetidinone and thiazolidinone derivatives." In PROCEEDINGS OF THE 3RD INTERNATIONAL CONFERENCE ON AUTOMOTIVE INNOVATION GREEN ENERGY VEHICLE: AIGEV 2018. Author(s), 2019. http://dx.doi.org/10.1063/1.5087379.

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Mangalagiu, Ionel, Violeta Mangalagiu, Costel Moldoveanu, Gheorghita Zbancioc, Ramona Danac, and Vasilichia Antoci. "Antimicrobial and anticancer activity of some hybrid azine/azole derivatives." In New frontiers in natural product chemistry, scientific seminar with international participation. Institute of Chemistry, 2021. http://dx.doi.org/10.19261/nfnpc.2021.ab07.

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Khachatryan, D. S., A. V. Kolotaev, V. N. Osipov, V. A. Yashkir, and K. R. Matevosyan. "Quaternary ammonium derivatives of 2-aminothiophene-3-carboxylates with antimicrobial activity." In PROCEEDINGS OF THE 3RD INTERNATIONAL CONFERENCE ON AUTOMOTIVE INNOVATION GREEN ENERGY VEHICLE: AIGEV 2018. Author(s), 2019. http://dx.doi.org/10.1063/1.5087355.

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