Yazar "Atas, Mehmet" seçeneğine göre listele

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    Öğe
    Aminopyrazole-substituted metallophthalocyanines: Preparation, aggregation behavior, and investigation of metabolic enzymes inhibition properties
    (Wiley-V C H Verlag Gmbh, 2019) Guzel, Emre; Kocyigit, Umit M.; Arslan, Baris S.; Atas, Mehmet; Taslimi, Parham; Gokalp, Faik; Gulcin, Ilhami
    The synthesis, characterization, aggregation behavior, theoretical studies, and investigation of antimicrobial, antidiabetic, and anticholinergic properties of 4-(2-(5-amino-4-(4-bromophenyl)-3-methyl-1H-pyrazol-1-yl)ethoxy)phthalonitrile (2) and its soluble aminopyrazole-substituted peripheral metallo (Mn, Co, and Ni)-phthalocyanine complexes (3-5) are reported for the first time. The synthesized compounds and phthalocyanine complexes were characterized spectroscopically. The new phthalonitrile derivative (2) and its peripheral metallophthalocyanine complexes (3-5) were found to be effective inhibitors of alpha-glycosidase, acetylcholinesterase (AChE), human carbonic anhydrase I and II isoforms (hCA I and II), and butyrylcholinesterase (BChE) with K-i values in the range of 1.55 +/- 0.47 to 10.85 +/- 3.43 nM for alpha-glycosidase, 8.44 +/- 0.32 to 21.31 +/- 7.91 nM for hCA I, 11.73 +/- 2.82 to 31.03 +/- 4.81 nM for hCA II, 101.62 +/- 26.58 to 326.54 +/- 89.67 nM for AChE, and 68.68 +/- 11.15 to 109.53 +/- 19.55 nM for BChE. This is the first study of peripherally substituted phthalocyanines containing an aminopyrazole group as potential carbonic anhydrase enzyme inhibitor. Also, the antimicrobial activities of the synthesized compounds were evaluated against six microorganisms (four bacteria and two Candida species) using the broth microdilution method. The gram-positive bacteria were detected to be more sensitive than gram-negative bacteria and yeasts in the synthesized compounds.
  • [ X ]
    Öğe
    Composition characterization and biological activity study of Thymbra spicata l. var. spicata essential oil
    (2021) Eruygur, Nuraniye; Kocyıgıt, Umit M.; Atas, Mehmet; Cevık, Ozge; Gökalp, Faik; Taslimi, Parham; Gulcın, İlhami
    The current research aimed to determine and report in vitro antioxidant, antimicrobial, antibiofilm, cytotoxic, anti-cholinesterase, and anti-diabetic properties and the stability of the major component of basic oil of Thymbra spicata var. spicata through different phases as theoretically. Essential oil exhibits potential biological activities because of the multiple components it contains.In the current research, the evaluation of Thymbra spicata essential oil antioxidant properties was conducted utilizing 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2- azinobis[3-ethylbenzthiazoline]-6-sulfonic acid (ABTS) radical scavenging activity.Antimicrobial activity was assessed from minimum inhibition concentration (MIC) using the technique of microdilution and cytotoxicity activity was evaluated by MTT assay through MCF-7 and PC3 human cancer cell lines.Consequently, Cytotoxic activity was evaluated by means of MTT assay utilized. The essential oil was detected to have 340 ?g/mL inhibiting influence on the growth of PC3 prostate cancer cells with IC50 value. Also, the T. spicata plant was observed to significantly repress the enzymes, namely acetylcholinesterase (AChE), butyrylcholinesterase (BChE), ?-glycosidase. IC50 values of enzymes were obtained 0.23 ?g/mL for AChE, 1.64 ?g/mL for BChE, 7.78 ?g/mL for ?-glycosidase. It was concluded that this plant may be used for Alzheimer's and diabetes disease.
  • [ X ]
    Öğe
    Functionalized methoxy quinoline derivatives: Experimental and in silico evaluation as new antiepileptic, anti-Alzheimer, antibacterial and antifungal drug candidates
    (Elsevier, 2024) Ciftci, Bilge; Okten, Salih; Kocyigite, Umit Muhammet; Atalay, Vildan Enisoglu; Atas, Mehmet; Cakmak, Osman
    The objective of this study was to assess the inhibitory effects of newly synthesized quinoline derivatives on human carbonic anhydrase I and II (hCA I and II), as well as acetylcholinesterase (AChE) enzymes, alongside their impact on various microorganisms. The synthesized compounds were assessed using IC50, Ki and MIC values via Ellman and Esterease Method and Microdilution assay. Most compounds exhibited strong inhibitory effects on human carbonic anhydrase I and II (hCA I and II) and acetylcholinesterase (AChE), notably compounds 9, 12, and 17 for hCA I, and 9, 12, 16 and 17 for hCA II, alongside robust AChE inhibition by compounds 8 and 13. Antimicrobial tests highlighted compounds 13 and 15 as promising inhibitors against pathogens, particularly effective across various strains. Molecular docking supported these findings, indicating potent binding abilities, notably by compounds 16 and 17 across specific protein structures (2COP, 5E2M, and 6KM3). The discussion emphasized the impact of substituents, particularly methoxy groups at specific positions, on enzyme inhibition, revealing how structural modifications affected enzyme inhibitory properties. The comprehensive analysis bridged experimental and computational findings, uncovering essential structure-activity relationships in quinoline derivatives and identifying potential candidates for further studies in enzyme inhibition and antimicrobial research.