Yazar "Bartolucci, Gianluca" seçeneğine göre listele

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    Preparation, carbonic anhydrase enzyme inhibition and antioxidant activity of novel 7-amino-3,4-dihydroquinolin-2(1H)-one derivatives incorporating mono or dipeptide moiety
    (Taylor & Francis Ltd, 2020) Kucukbay, Hasan; Gonul, Zeynep; Kucukbay, F. Zehra; Angeli, Andrea; Bartolucci, Gianluca; Supuran, Claudiu T.
    New dipeptide-dihydroquinolinone derivatives were successfully synthesised by benzotriazole mediated nucleophilic acyl substitution reaction and their structures were elucidated by spectroscopic and analytic techniques. The carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activity of the new compounds was determined against four human (h) isoforms, hCA I, hCA II, hCA IX and hCA XII. While all compounds showed moderate to good in vitro CA inhibitory properties against hCA IX and hCA XII with inhibition constants in the micromolar level (37.7-86.8 and 2.0-8.6 mu M, respectively), they did not show inhibitory activity against hCA I and hCA II up to 100 mu M concentration. The antioxidant capacity of the peptide-dihydroquinolinone conjugates was determined using 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging method. Most of the synthesised compounds showed low antioxidant activities compared to the control antioxidant compounds BHA and alpha-tocopherol.
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    Synthesis and carbonic anhydrase inhibitory properties of novel 4-(2-aminoethyl)benzenesulfonamide-dipeptide conjugates
    (Academic Press Inc Elsevier Science, 2019) Kucukbay, Hasan; Bugday, Nesrin; Kucukbay, F. Zehra; Berrino, Emanuela; Bartolucci, Gianluca; Del Prete, Sonia; Capasso, Clemente
    Thirty novel sulfonamide derivatives incorporating dipeptide were synthesized by facile acylation through benzotriazole mediated reactions and their structures were identified by H-1 NMR, C-13 NMR, MS and FT-IR spectroscopic techniques and elemental analysis. The carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activity of the new compounds was assessed against four human (h) isoforms, hCA I, hCA II, hCA IV and hCA XII. Most of the synthesized compounds showed excellent in vitro carbonic anhydrase inhibitory properties comparable to those of the clinically used drug acetazolamide (AAZ). The new unprotected dipeptide-sulfonamide conjugates showed very effective inhibitory activity, in the low nanomolar range against II and XII, being less effective as hCA I and IV inhibitors. Four of the thirty compounds also showed strong inhibitory activity against hCA XII compared to AAZ.
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    Synthesis and human carbonic anhydrase I, II, VA, and XII inhibition with novel amino acid-sulphonamide conjugates
    (Taylor & Francis Ltd, 2020) Kucukbay, Hasan; Bugday, Nesrin; Kucukbay, F. Zehra; Ageli, Andrea; Bartolucci, Gianluca; Supuran, Claudiu T.
    A series of amino acid-sulphonamide conjugates was prepared through benzotriazole mediated coupling reactions and characterised by H-1-NMR, C-13-NMR, MS, and FTIR spectroscopic techniques as well as elemental analysis. The carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activity of the new compounds was determined against four human (h) isoforms, hCA I, hCA II, hCA VA, and hCA XII. Most of the synthesised compounds showed effective in vitro CA inhibitory properties. The new amino acid-sulphonamide conjugates showed potent inhibitory activity against hCA II, some of them at subnanomolar levels, exhibiting more effective inhibitory activity compared to the standard drug acetazolamide. Some of these sulphonamides were also found to be effective inhibitors of hCA I, hCA VA, and hCA XII, with activity from the low to high nanomolar range.
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    Synthesis of new 7-amino-3,4-dihydroquinolin-2(1H)-one-peptide derivatives and their carbonic anhydrase enzyme inhibition, antioxidant, and cytotoxic activities
    (Wiley-V C H Verlag Gmbh, 2021) Kucukbay, Hasan; Gonul, Zeynep; Kucukbay, Fatumetuzzehra Zehra; Tekin, Zehra; Angeli, Andrea; Bartolucci, Gianluca; Supuran, Claudiu T.
    Six new monopeptides, seven new dipeptides, and two deprotected monopeptide dihydroquinolinone conjugates were prepared by the benzothiazole-mediated method and their structures were confirmed by nuclear magnetic resonance, mass, infrared spectroscopy, and elemental analysis methods. The human carbonic anhydrase (hCA) I and hCA II enzyme inhibition activities of the compounds were determined using the stopped-flow instrument. The synthesized peptide-dihydroquinolinone conjugates 2, 3, 6, 10, 13, and 15 showed inhibition against the hCA II enzyme in the range of 15.7-65.7 mu M. However, none of the compounds showed inhibition of hCA I at a concentration of 100 mu M. The antioxidant activities of the compounds were also examined using the DPPH (2,2-diphenyl-1-picrylhydrazyl) radical scavenging method at concentrations of 12.5-125 mu g/ml, but when compared with the standard antioxidant compounds alpha-tocopherol and butylated hydroxyanisole (BHA), weak antioxidant activities were detected. The cytotoxic effects of four compounds against the A549 and BEAS-2B cell lines were also investigated. Among the compounds studied, compound 7 was found to be most effective, with the IC50 values on the A549 cells for 48 and 72 h being 26.87 and 9.979 mu g/ml, respectively, and the IC50 values on the BEAS-2B cells being >100 mu g/ml. None of the tested compounds showed antimicrobial activity in the concentration range (800-1.56 mu g/ml) studied.
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    Synthesis of novel dipeptide sulfonamide conjugates with effective carbonic anhydrase I, II, IX, and XII inhibitory properties
    (Academic Press Inc Elsevier Science, 2018) Bugday, Nesrin; Kucukbay, F. Zehra; Kucukbay, Hasan; Bua, Silvia; Bartolucci, Gianluca; Leitans, Janis; Kazaks, Andris
    Twenty-four novel sulfonamide derivatives incorporating dipeptide tails were synthesized by facile acylation reactions of homosulfanilamide through benzotriazole or dicyclohexyl carbodiimide (DCC) mediated coupling reactions. The carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activity of the new compounds was assessed against four human (h) isoforms, hCA I, hCA II, hCA IX and hCA XII. Most of the synthesized compounds showed good in vitro carbonic anhydrase inhibitory properties, with inhibition constants in the low nanomolar range. Particularly, the new dipeptide-sulfonamide conjugates incorporating Ala, Phe and met in the dipeptide sequence, showed the most effective inhibitory activity against to CA IX and XII.
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    Synthesis, antioxidant and carbonic anhydrase inhibitory properties of monopeptide-anthraquinone conjugates
    (Acg Publications, 2021) Kucukbay, Hasan; Parladi, F. Muzeyyen; Kucukbay, F. Zehra; Angeli, Andrea; Bartolucci, Gianluca; Supuran, Claudiu T.
    Novel monopeptide-anthraquinone conjugates (1-16) were synthesized by the reaction of appropriate N-protected amino acid with 2-hydroxymethylanthraquinone in good or high yields. The structural elucidation of the new compounds was accomplished by H-1 NMR, C-13 NMR, MS, FT-IR spectroscopy and elemental analysis techniques. The carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activity of the new compounds was determined against two human (h) isoforms, hCA I and hCA II. While three of the sixteen compounds showed moderate in vitro carbonic anhydrase inhibitory properties against hCA II with inhibition constants in the micromolar level (43.5, 67.4 and 78.1 mu M), they did not show inhibitory activity against hCA I up to 100 mu M concentration. The antioxidant abilities of the compounds were determined using the 1,1-diphenyl-2-picrylhydrazil (DPPH) radical scavenging method, ferric ion reducing assay and metal chelation methods. While a small amount of antioxidant activity was observed according to the DPPH and ferric ion reducing power assay methods, none of the compounds showed antioxidant properties according to the metal chelating activity method at the concentrations studied.