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    Öğe
    Preparation, structural analysis, bioactivity assessment, enzyme and molecular docking calculations of some furan/thiophene-2-carboxamide derivatives
    (Springer, 2023) Cakmak, Sukriye; Yenigun, Semiha; Ozen, Tevfik
    Some furan/thiophene-2-carboxamide derivatives (1-3) were prepared from acyl chlorides and heterocyclic amine derivatives with good yields, employing synthetic route and their chemical structures were confirmed using different spectroscopic methods including IR, 1H NMR, 13C NMR and elemental analysis. Three different enzyme inhibition effect tests as urease, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibiting activities, were applied to these compounds. The biological evaluation results clearly showed that the compound 1 showed approximately 9.8-fold more activity against urease enzyme than thiourea standard while the compound 3 showed approximately 4.2-fold more activity against BChE enzyme than galantamine standard. The molecular interaction for each of the target compounds with the active sites of the urease, acetylcholinesterase and butyrylcholinesterase enzymes was investigated by molecular insertion simulations and the results were confirmed the experimental findings. The results also show that compounds such as 1 and 3 carrying thiophene/furan carbocamide moieties could be used promising structures in the development of more potent pharmaceutical agents in the future.
  • [ X ]
    Öğe
    Synthesis, characterization, antioxidant, and antibacterial activities of new 2,3-dimethoxy and 3-acetoxy-2-methyl benzamides
    (Springer, 2020) Yakan, Hasan; Cakmak, Sukriye; Kutuk, Halil; Yenigun, Semiha; Ozen, Tevfik
    We performed a series of novel benzamide compounds which were synthesized starting from 2,3-dimethoxybenzoic acid or 3-acetoxy-2-methylbenzoic acid and amine derivatives. All the obtained products were purified, and the analysis of these products was determined with IR, H-1 NMR, C-13 NMR spectroscopic, and elemental methods. The in vitro antioxidant activity of all the compounds was determined by total antioxidant, free radical scavenging, and metal chelating activity. Some of synthesized compounds showed more effective total antioxidant, free radical scavenging, and metal chelating activity compared with standards. One of the benzamide compounds has been shown to exhibit effective metal chelate activity. The new compounds were determined in vitro antibacterial activity against three gram-positive bacteria and three gram-negative bacteria and compared with two control drugs. Thus, by conducting in vivo biochemical tests of effective amides, researches can be carried out in different fields of application. Graphic abstract We performed a series of novel benzamide compounds which were synthesized, and the analysis of these products was determined with IR, H-1 NMR, C-13 NMR spectroscopic, and elemental methods. The in vitro antioxidant activity of all the compounds was determined by total antioxidant, free radical scavenging, and metal chelating activity. All the compounds were tested for their in vitro growth inhibitory activity against different bacteria.
  • [ X ]
    Öğe
    The enzyme kinetic studies, DNA protection and antioxidant activities of furan/ thiophene-2-carboxamide derivatives
    (Ibrahim DEMIRTAS, 2024) Çakmak, Sükriye; Yenigün, Semiha; Ozen, Tevfik
    Three furan and/or thiophene-2-carboxamide compounds, namely N-(furan-2-ylmethyl)thiophene-2-carboxamide (1), N-(furan-2-carbonyl)furan-2-carboxamide (2), and N-(Thiophene-2-ylmethyl)furan-2-carboxamide (3) were investigated the enzyme kinetic studies by urease, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE). The inhibition constant (Ki) of Compound (CPD)3 by AChE was determined as 0.10 mM, and the Ki value by BChE was determined as 0.07 mM. In comparison, the Ki value of CPD1 by urease was determined as 0.10 mM. These CPDs were examined for antioxidant activity by the DPPH? scavenging method. CPD3 exhibited 98.93% DPPH scavenging activity compared to ascorbic acid, the positive control group. Furthermore, the DNA-protective activities of the compounds were investigated, and the DNA protection activity of CPD1 was observed to be 78%. The findings suggest that thiophene/furan carboxy amide-containing CPD1 and CPD3 might be exploited as potential structures for evaluating pharmaceuticals with greater potency.