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    Dimethoxyindoles based thiosemicarbazones as multi-target agents; synthesis, crystal interactions, biological activity and molecular modeling
    (Academic Press Inc Elsevier Science, 2022) Yildiz, Minhal; Bingul, Murat; Zorlu, Yunus; Saglam, Mehmet F.; Boga, Mehmet; Temel, Mutesir; Koca, Mehmet Serdar
    Alzheimer's disease (AD) is known as one of the most devastating neurodegenerative disease diagnosed for the old-aged people and cholinesterase inhibitors (ChEI) can be used as an effective palliative treatment for AD. A range of novel monomeric and dimeric indole based thiosemicarbazone derivatives 17-28 was synthesized in order to target cholinesterases (ChE). Biological importance of the targeted compounds 17-28 was investigated by employing the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes along with three different antioxidant property determination assays, namely DPPH free radical scavenging, ABTS cationic radical decolarization, and CUPRAC cupric reducing antioxidant capacity. The compounds 18 and 19 displayed the best inhibitor activity against BChE with IC50 values of 7.42 and 1.95 mu M, respectively. The antioxidant potentials were found to be moderate for DPPH and ABTS assays and the compounds 28 and 18 were the most potent candidates for both antioxidant assays. Cupric reducing capacity was the most promising assay and the compounds 25, 26 and 28 provided better inhibition values than all the standards. Further binding mode and affinity studies performed by molecular docking and molecular dynamics simulations. Accordingly, the compound 19 is the most plausible candidate that can compete with galantamine (GNT), a common pharmaceutics targeting both cholinesterase enzymes.
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    Öğe
    Synthesis and molecular modeling studies of naphthazarin derivatives as novel selective inhibitors of ?-glucosidase and ?-amylase
    (Elsevier B.V., 2023) Abadan, Şebnem; Sağlam, Mehmet F.; Koca, Mehmet Serdar; Bingül, Murat; Şahin, Hasan; Zorlu, Yunus; Şengül, İbrahim F.
    Diabetes mellitus is known as one of the most life-threatening diseases and has attracted the attention of medicinal chemists. The design and synthesis of novel potential candidates for the inhibition of αamylase and α-glucosidase enzymes which are responsible for the digestion of dietary carbohydrates are an important approach for the treatment of diabetes. In this current work, a range of novel mono and naphthazarin derivatives were successfully synthesized by the esterification reaction of naphthazarin with different benzoyl chlorides and heterocyclic acyl chlorides. The synthesized compounds were subjected to in vitro antidiabetic activities through α-glucosidase and α-amylase inhibition properties. Despite the limited inhibition potential against α-amylase enzymes, naphthazarin derivatives would be promising targets for antidiabetic study due to the specificity for α-glucosidase enzyme. The compound 18 revealed a dual inhibition behavior, however all the other active compounds were detected as specific for α-glucosidase inhibition and quite potent compared to the standard acarbose which is promising for eliminating the side effects associated with the non-selectivity of acarbose. The compound 19 was the best candidate for inhibition with IC50 value of 7.4 μM and resulted 150-fold better activity compared to the standard. Free energy calculations support the experimental binding affinity of compound 19 found as the most promising drug candidate for α-glucosidase among the synthesized compounds. The plausible binding mode and the interaction of compound 19 complexed with α-glucosidase has been revealed by MD simulations.
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    Öğe
    Synthesis, characterization, UV-Vis absorption and cholinesterase inhibition properties of bis-indolyl imine ligand systems
    (Elsevier, 2020) Saglam, Mehmet F.; Bingul, Murat; Senkuytu, Elif; Boga, Mehmet; Zorlu, Yunus; Kandemir, Hakan; Sengul, Ibrahim F.
    A number of bis-indolyl imine helical structures has successfully been synthesized employing Schiff base reaction conditions starting from 4,6-dimethoxy-2,3-diphenylindole with different o-phenyl diamines as pi-spacer bridged. The structures of targeted compounds were identified by FT-IR, mass, H-1 and C-13 NMR spectroscopy along with single crystal X-ray diffraction techniques. The ground state absorption properties of the bis-indolyl compounds were also investigated utilizing UV-Vis absorption spectroscopy. As the biological aspect of the synthesized compounds, the anticholinesterase potency was investigated towards the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. The highest inhibition was determined in the presence of compound 9 with the values of 89.21 and 96.06, better than standard Galantamine, for AChE and BChE, respectively. (C) 2020 Elsevier B.V. All rights reserved.