1,721,049 research outputs found
Synthesis, characterization, biological evaluation, and in silico studies of novel 1,3-diaryltriazene-substituted sulfathiazole derivatives
No full textISIK, MESUT/0000-0002-4677-8104; Gulcin, ilhami/0000-0001-5993-1668WOS: 000539602200001PubMed: 32529657In the present study, a series of eleven novel 1,3-diaryltriazene-substituted sulfathiazole moieties (ST1-11) was synthesized by the reaction of diazonium salt of sulfathiazole with substituted aromatic amines and their chemical structures were characterized by Fourier transform infrared,H-1-NMR (nuclear magnetic resonance),C-13-NMR, and high-resolution mass spectroscopy methods. These synthesized novel derivatives were found to be effective inhibitor molecules for alpha-glycosidase (alpha-GLY), human carbonic anhydrase (hCA), and acetylcholinesterase (AChE), withK(I)values in the range of 426.84 +/- 58.42-708.61 +/- 122.67 nM for alpha-GLY, 450.37 +/- 50.35-1,094.34 +/- 111.37 nM forhCA I, 504.37 +/- 57.22-1,205.36 +/- 195.47 nM forhCA II, and 68.28 +/- 10.26-193.74 +/- 19.75 nM for AChE. Among the synthesized novel compounds, several lead compounds were investigated against the tested metabolic enzymes. More specifically,ST11(4-[3-(perfluorophenyl)triaz-1-en-1-yl]-N-(thiazol-2-yl)benzenesulfonamide) showed a highly efficient inhibition profile againsthCA I,hCA II, and AChE, withK(I)values of 450.37 +/- 50.35, 504.37 +/- 57.22, and 68.28 +/- 10.26 nM, respectively. Due to its significant biological inhibitory potency, this derivative may be considered as an interesting lead compound against these enzymes.Research Fund of Anadolu UniversityAnadolu University [1610S681]Research Fund of Anadolu University, Grant/Award Number: 1610S68
Synthesis, cytotoxicities, and carbonic anhydrase inhibition potential of 6-(3-aryl-2-propenoyl)-2(3H)-benzoxazolones
Full text linkGULCIN, Ilhami/0000-0001-5993-1668; Sakagami, Hiroshi/0000-0001-8001-2121; Bilginer, Sinan/0000-0001-5676-2045; Supuran, Claudiu/0000-0003-4262-0323WOS: 000488460400001PubMed: 31576761In this study, new chalcone compounds having the chemical structure of 6-(3-aryl-2-propenoyl)-2(3H)-benzoxazolones (1?8) were synthesised and were characterised by H-1-NMR, C-13?-NMR, and HRMS spectra. Cytotoxic and carbonic anhydrase (CA) inhibitory effects of the compounds were investigated. Cytotoxicity results pointed out that compound 4, 6-[3-(4-trifluoromethylphenyl)-2-propenoyl]-3H-benzoxazol-2-one, showed the highest cytotoxicity (CC50) and potency-selectivity expression (PSE) value, and thus can be considered as a lead compound of this study. According to the CA inhibitory results, IC50 values of the compounds 1?8 towards hCA I were in the range of 29.74?69.57??M, while they were in the range of 18.14 ? 48.46??M towards hCA II isoenzyme. K-i values of the compounds 1?8 towards hCA I were in the range of 28.37???6.63?70.58???6.67??M towards hCA I isoenzyme and they were in the range of 10.85???2.14 ? 37.96???2.36??M towards hCA II isoenzyme.Ataturk University Research FundAtaturk University [2016/118]This research was supported by the Ataturk University Research Fund (Project number: 2016/118)
Ostr. (Apiaceae)
No full textGulcin, ilhami/0000-0001-5993-1668; KARAKAYA, Songul/0000-0002-3268-721XWOS: 000524099800001The oxidant, cholinesterase, and carbonic anhydrase inhibitions of essential oils and their major compounds of Leiotulus dasyanthus and molecular docking studies of alpha-pinene and (TM)-3-carene were evaluated in this study. Phenolic constituents and antioxidant activity of samples were determined by Folin-Ciocalteu's, DPPH, and TBA processes. Cholinesterase inhibition effect was evaluated through Ellman's method. GC-FID and GC/MS were used for analysing of essential oils. the root oil got the highest total phenolic content (898.87 mg/g). the utmost activity was shown flower oil (29.31 mu g/mL) in the DPPH test. the root oil indicated considerable inhibition towards acetylcholinesterase (21.92%) and butyrylcholinesterase (91.33%) enzymes, respectively. alpha-pinene and delta-3-carene indicated high acetylcholinesterase inhibitory activity (66.44 and 48.71%, respectively). Cytosolic hCA I and II isoenzymes were influentially inhibited by flower and aerial part oils with 1.694 and 1.677 mu M IC50 values, respectively. 1-Dodecanol (7.8%); beta-pinene (63.3%), alpha-pinene (20.5%); octyl acetate (14.7%); hexyl octanoate (55.1%) were characterized as principle compounds of aerial parts, roots, flowers, and fruits respectively.Ataturk UniversityAtaturk University [TAB-2018-6432]This work was assisted by the Scientific Research Projects of Ataturk University (TAB-2018-6432).Scientific Research Projects of Ataturk University (TAB-2018-6432)
Going Beyond Counting First Authors in Author Co-citation Analysis
Full text linkThe present study examines one of the fundamental aspects of author co-citation analysis (ACA) - the way co-citation
counts are defined. Co-citation counting provides the data on which all subsequent statistical analyses and mappings
are based, and we compare ACA results based on two different types of co-citation counting - the traditional type that
only counts the first one among a cited work's authors on the one hand and a non-traditional type that takes into
account the first 5 authors of a cited work on the other hand. Results indicate that the picture produced through this non-traditional author co-citation counting contains more coherent author groups and is therefore considerably clearer. However, this picture represents fewer specialties in the research field being studied than that produced through the traditional first-author co-citation counting when the same number of top-ranked authors is selected and analyzed. Reasons for these effects are discussed
Measurement of antioxidant ability of melatonin and serotonin by the DMPD and CUPRAC methods as trolox equivalent
No full textMelatonin (N-acetyl-5-methoxytryptamine) is the chief secretory product of the pineal gland and synthesized enzymatically from serotonin (5-hydroxytryptamine). These indoleamine derivatives play an important role in the prevention of oxidative damage. In the present study, DMPD radical scavenging and cupric ion (Cu2+) reducing ability of melatonin and serotonin as trolox equivalent antioxidant activity (TEAC) was investigated. Melatonin and serotonin demonstrated 73.5 and 127.4g/mL trolox equivalent DMPD+ scavenging activity at the concentration of 100g/mL. Also, at the same concentration, melatonin and serotonin showed 14.41 and 116.09g/mL trolox equivalent cupric ion (Cu2+) reducing ability. These results showed that melatonin and serotonin had marked DMPD+ radical scavenging and cupric ions (Cu2+) reducing ability. Especially, serotonin had higher DMPD radical scavenging and cupric ions (Cu2+) reducing activity than melatonin because of its phenolic group
Variations on the Author
Full text link“Variations on the Author” discusses two of Eduardo Coutinho’s recent films (Um Dia na Vida, from 2010, and Últimas Conversas, posthumously released in 2015) and their contribution to the general question of documentary authorship. The director’s filmography is characterized by a consistent yet self-effacing form of authorial self-inscription: Coutinho often features as an interviewer that rather than express opinions propels discourses; an interviewer that is good at listening. This mode of self-inscription characterizes him as an author who is not expressive but who is nonetheless markedly present on the screen. In Um Dia na Vida, however, Coutinho is completely absent form the image, while Últimas Conversas, on the contrary, includes a confessional prologue that moves the director from the margins to the center of his films. This article examines the ways in which these works stand out in the filmography of a director who offers new insights into the notion of cinematic authorship
Appropriate Similarity Measures for Author Cocitation Analysis
Full text linkWe provide a number of new insights into the methodological discussion about author cocitation analysis. We first argue that the use of the Pearson correlation for measuring the similarity between authors’ cocitation profiles is not very satisfactory. We then discuss what kind of similarity measures may be used as an alternative to the Pearson correlation. We consider three similarity measures in particular. One is the well-known cosine. The other two similarity measures have not been used before in the bibliometric literature. Finally, we show by means of an example that our findings have a high practical relevance.information science;Pearson correlation;cosine;similarity measure;author cocitation analysis
Dispelling the Myths Behind First-author Citation Counts
Full text linkWe conducted a full-scale evaluative citation analysis study of scholars in the XML research field to explore just how different from each other author rankings resulting from different citation counting methods actually are, and to demonstrate the capability of emerging data and tools on the Web in supporting more realistic citation counting methods. Our results contest some common arguments for the continued
use of first-author citation counts in the evaluation of scholars, such as high correlations between author rankings by first-author citation counts and other citation
counting methods, and high costs of using more realistic citation counting methods that are not well-supported by the ISI databases. It is argued that increasingly available digital full text research papers make it possible for citation analysis studies to go beyond what the ISI databases have directly supported and to employ more
sophisticated methods
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