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  • Küçük Resim
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    Synthesis and Biological Evaluation of Novel Dihydro [2,3D] Pyridine Substituted Enaminosulfonamide Compounds as Potent Human Erythrocyte Carbonic Anhydrase II (hCAII) Inhibitors
    (2021) Demirci, Tuna; Özdemir, Oğuzhan; Kaya, Mustafa Oğuzhan; Arslan, Mustafa
    Dihydro [2,3D] pyridine substituted enaminosulfonamide compounds have been synthesizedand their effects on carbonic anhydrase II (hCAII) have been evaluated. Pyrido [2,3 d] pyrimidines were synthesized from barbituric acid derivatives, malonanitrile, aldehyde derivatives inbasic condition and then hydrolyzed with hydrochloric acid. The targeted compounds were synthesized from amino sulfanilamide, dihydro [2,3D] pyridine compounds, and triethylorthoformate. 1H NMR, 13C NMR, FT-IR and elemental analysis were used for the structural analysisof the compounds. The half maximal inhibitory concentration (IC50) values of the compoundswere determined to be between 27.03 and 104.39 ?M for hCA II and 19.85-76.64 ?M for Ki.
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    Öğe
    Synthesis, inhibition effects, molecular docking and theoretical studies as Paraoxonase 1 (PON1) inhibitors of novel 1,4-dihydropyridine substituted sulfonamide derivatives
    (Springer Birkhauser, 2023) Kaya, Mustafa Oguzhan; Demirci, Tuna; Özdemir, Oğuzhan; Çalışır, Ümit; Sönmez, Fatih; Arslan, Mustafa
    The novel sulfonamide substitute 1,4-dihydropyridine derivatives were synthesized by the method of Hantzsch reaction. They have been characterized by FT-IR spectroscopy, H-1-NMR, C-13-NMR, and elemental analysis. PON1 which is an antioxidant enzyme has important functions in cardiovascular systems. The enzyme has been purified using a two-step method such as ammonium sulfate precipitation and sepharose-4B-l-tyrosine-9-aminophenanthrene hydrophobic interaction chromatography. The results demonstrated that all the synthesized compounds inhibited PON1 enzyme. The best inhibition effect was observed in compound (1) for PON1 enzyme (IC50: 8.04 mu M, K-i: 5.43 mu M). The free radical scavenging for PON1 was discovered as 20.16 mg/mL, while drug score value was reported as 0.13 for compound (1). Furthermore, the lowest binding energy (-1.31 kcal/mol) determined by molecular docking for PON1 enzyme and the lowest LUMO-HOMO gap ( increment E = 3.12 eV) were calculated for compound (1).