Yazar "Arslan, Mustafa" seçeneğine göre listele

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    Öğe
    IN VITRO EFFECTS OF NEW GENERATION BISOXADIAZOLE SUBSTITUTED SULFONAMIDE DERIVATIVES ON HUMAN SERUM PARAOXONASE1 (PON1)
    (Parlar Scientific Publications (P S P), 2018) Kaya, Mustafa Oguzhan; Gulec, Ozcan; Arslan, Mustafa
    In this study, new bisoxadiazole substituted sulfonamide compounds were synthesized and in vitro inhibition effects of the compouds on purified human serum paraoxonase 1 (PON I) were investigated by using the method of Gan et al. The results showed that all the synthesized compounds inhibited the paraoxonase 1 enzyme activity. The compounds 6d and 6e were found to be most active compounds (IC50=26.5 mu M and 28.6 mu M) for PON1, respectively.
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    Öğe
    In vitro inhibition of purified human carbonic anhydrase I and II by novel fluorene derivatives
    (Macedonian Journal of Chemistry and Chemical Engineering, 2014) Demirhan, Hulya; Arslan, Mustafa; Kaya, Mustafa Oguzhan; Kaya, Yesim; Gencer, Nahit; Arslan, Oktay
    In this study, 9-benzylidene-9H-fluorene-substituted urea (5a-p) and thiourea derivatives (5q-v) were synthesized and their inhibitory effects on the activity of human carbonic anhydrase (hCA) I and II were evaluated. hCA I and II were purified from human erythrocytes using a Sepharose 4B-L-tyrosine-sulphanilamide affinity column. All the synthesized compounds inhibited the activity of the hCA I and II isoenzymes. Among the synthesized compounds, 5f was found to be the most active (IC50 = 21.4 ?M) for inhibition of hCA I and 5s was the most active (IC50 = 25.3 ?M) for inhibition of hCA II.
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    Öğe
    IN VITRO INHIBITION OF PURIFIED HUMAN CARBONIC ANHYDRASE I AND II BY NOVEL FLUORENE DERIVATIVES
    (Soc Chemists Technologists Madeconia, 2014) Demirhan, Hulya; Arslan, Mustafa; Kaya, Mustafa Oguzhan; Kaya, Yesim; Gencer, Nahit; Arslan, Oktay
    In this study, 9-benzylidene-9H-fluorene-substituted urea (5a-p) and thiourea derivatives (5q-v) were synthesized and their inhibitory effects on the activity of human carbonic anhydrase (hCA) I and II were evaluated. hCA I and II were purified from human erythrocytes using a Sepharose 4B-L-tyrosine-sulphanilamide affinity column. All the synthesized compounds inhibited the activity of the hCA I and II isoenzymes. Among the synthesized compounds, 5f was found to be the most active (IC50 = 21.4 mu M) for inhibition of hCA I and 5s was the most active (IC50 = 25.3 mu M) for inhibition of hCA II.
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    Synthesis and carbonic anhydrase inhibitory properties of tetrazole- and oxadiazole substituted 1,4-dihydropyrimidinone compounds
    (Informa Healthcare, 2014) Celik, Fatma; Arslan, Mustafa; Kaya, Mustafa Oguzhan; Yavuz, Emre; Gencer, Nahit; Arslan, Oktay
    A new series of tetrazole-, oxadiazole-and cyanosubstituted 1,4-dihydropyrimidinone compounds were synthesized, and their inhibitory effects on the activity of purified human carbonic anhydrase (hCA) I were evaluated. 4-Cyanophenyl-1,4- dihydropyrimidinone compounds were prepared with 1,3-diketone, cyanobenzaldehyde and urea. The compounds were reacted with sodium azide and then with anhydride to get the final products. The results showed that all the synthesized compounds inhibited the CA isoenzyme activity. The compound 4-(1,7,7-trimethyl-2,5-dioxo-1,2,3,4,5,6,7,8-octahydroquinazoline- 4-yl) benzonitrile 6c (IC50 = 0.0547 mM) has the most inhibitory effect.
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    Öğe
    Synthesis, activatory effects, molecular docking and ADME studies as rabbit muscle pyruvate kinase activators of ureido phenyl substituted 1,4-dihydropyridine derivatives
    (Springer, 2024) Kaya, Mustafa Oguzhan; Demirci, Tuna; Calisir, Umit; Ozdemir, Oguzhan; Kaya, Yesim; Arslan, Mustafa
    In this study, the activation of pyruvate kinase enzyme in vitro via different urea substituents in the para position as functional groups of 1,4-dihydropyridine derivatives synthesized by Hantzsch reaction method was investigated. Elemental analysis, 1H-NMR, 13C-NMR and FT-IR spectroscopy were used to identify the ureido phenyl substituted 1,4-dihydropyridine derivatives. Virtual screening based on molecular docking supported the results of possible in vitro pyruvate kinase (PK) activators among the synthesized substances. The results showed that all compounds successfully activated PK. The strongest activator effect was shown by ethyl-4-(4-(4-(3-(3-methoxyphenyl)thioureido)phenyl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,7,8-hexahydroquinolin-3 (7) with an AC50 value of 87.70 mu M. In molecular docking studies, full compatibility (- 3016.93 FF), binding affinities (Delta G = - 8.58 kcal/mol), LUMO-HOMO energy gap (Delta E = 7.85 eV) in Density functional theory (DFT) studies and drug similarity score of the compounds were found to be 0.69. These results shed light on the therapeutic potential of the produced compounds to treat PK-related diseases.
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    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; Ozdemir, Oguzhan; Calisir, Umit; Sonmez, 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).