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    Synthesis, anticonvulsant and antimicrobial activities of some new 2-acetylnaphthalene derivatives
    (Pergamon-Elsevier Science Ltd, 2010) Karakurt, Arzu; Ozalp, Meral; Isik, Samil; Stables, James P.; Dalkara, Sevim
    In this study, as a continuation of our research for new (arylalkyl) imidazole anticonvulsant compounds, the design, synthesis and anticonvulsant/antimicrobial activity evaluation of a series of 2-acetylnaphthalene derivatives have been described. Molecular design of the compounds has been based on the modification of nafimidone [1-(2-naphthyl)-2-(imidazol-1-yl)ethanone], which is a representative of the (arylalkyl) imidazole anticonvulsant compounds as well as its active metabolite, nafimidone alcohol (3, 4). In general, these compounds were variously substituted at the alkyl chain between naphthalene and imidazole rings and subjected to some other modifications to evaluate additional structure-activity relationships. The anticonvulsant activity profile of those compounds was determined by maximal electroshock seizure (MES) and subcutaneous metrazol (scM) seizure tests, whereas their neurotoxicity was examined using rotarod test. All the ester derivatives of nafimidone alcohol (5a-h), which were designed as prodrugs, showed anticonvulsant activity against MES-induced seizure model. Four of the most active compounds were chosen for further anticonvulsant evaluations. Quantification of anticonvulsant protection was calculated via the ip route (ED(50) and TD(50)) for the most active candidate (5d). Observed protection in the MES model was 38.46 mg kg (1) and 123.83 mg kg (1) in mice and 20.44 mg kg (1), 56.36 mg kg (1) in rats, respectively. Most of the compounds with imidazole ring also showed antibacterial and/ or antifungal activities to a certain extent in addition to their anticonvulsant activity. (C) 2010 Elsevier Ltd. All rights reserved.
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    Synthesis, Anticonvulsant and Antimicrobial Activities of Some New [1-(2-Naphthyl)-2-(pyrazol-1-yl)ethanone]oxime Ethers
    (Bentham Science Publ Ltd, 2015) Ozdemir, Zeynep; Karakurt, Arzu; Calis, Unsal; Gunal, Selami; Isik, Samil; Sahin, Z. Sibel; Dalkara, Sevim
    In this study, 12 new oxime ether derivatives, which were expected to show anticonvulsant and antimicrobial activities, were synthesized. Oxime ether derivatives were synthesized by the reaction of various alkyl halides with 1-(2-naphthyl)- 2-(pyrazol-1-yl)ethanone oxime. Anticonvulsant activity of the compounds was determined by maximal electroshock (MES) and subcutaneous metrazol (ScM) seizure tests, while neurological disorders were evaluated using rotorod toxicity test according to the ASP of NIH. Compound 1, 6 and 7 showed anticonvulsant activity at 300 mg/kg dose at 4 h, but compounds 1 and 7 showed toxicity at 300 mg/kg dose at half an hour. Antimicrobial activities of the compounds were also determined using agar microdilution method. Compound 1 and 5 were found to have the highest antifungal activity among the other compounds.
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    An X-ray and DFT Computational Study on 1-(Naphthalene-2-yl)-2-(1H-pyrazol-1-yl) ethanone O-butyl Oxime
    (Elsevier, 2012) Sahin, Zarife Sibel; Ozdemir, Zeynep; Karakurt, Arzu; Isik, Samil
    The title compound, 1-(naphthalene-2-yl)-2-(1H-pyrazol-1-yl)ethanone O-butyl oxime, I, was synthesized. The crystal and molecular structures of I were determined by IR, H-1-NMR, mass spectrum, elemental analysis and X-ray single crystal diffraction. Molecular geometry from X-ray experiment of I in the ground state was compared using the Density Functional Theory (DFT) with B3LYP/6-311G(d,p) basis set. In addition, DFT calculation, molecular electrostatic potentials (MEP) and frontier molecular orbitals of I were performed at the B3LYP/6-311G(d,p) level of the theory.