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    Synthesis and anticonvulsant activity of some alkanamide derivatives
    (2010) Tarikogullari A.H.; Kilic F.S.; Erol K.; Pabuccuoglu V.
    A group of N -phenylacetamide, N-phenylpropanamide and N-benzylamide derivatives bearing 5-membered heterocyclic rings such as pyrazole, 1,2,4-triazole and imidazole rings at ? position were synthesized and their anticonvulsant activity was evaluated in the maximal electroshock test. The results indicated that the 1,2,4-triazole ring leads to superior activity than the pyrazole ring and inserting a CH2 group into the anilide structure leading to N-benzyl derivatives did not change the anticonvulsant activity, but caused a noticeable decrease in duration of action. The most active compound was 2-(1H-1,2,4-triazole-1-yl)-N-(2,6-dimethylphenyl)acetamide. © ECV · Editio Cantor Verlag.
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    Synthesis and cytotoxic activity of some 2-(2,3-dioxo-2,3-dihydro-1H-indol- 1-yl)acetamide derivatives
    (2013) Akgül O.; Tarikogullari A.H.; Köse F.A.; Kirmizibayrak P.B.; Pabuççuoglu M.V.
    Isatin, 1H -indoline-2,3-dione, an endogenous compound, is also a synthetically versatile molecule that possesses a diversity of biological activities including anticonvulsant, antibacterial, antifungal, antiviral, anticancer, and cytotoxic properties. Based on the promising cytotoxic activity studies on N -substituted isatin derivatives, a series of 18 derivatives of 2-(2,3-dioxo-2,3-dihydro-1H -indol-1-yl)-N-phenylacetamide were designed, synthesized, and characterized according to their analytical and spectral data. All of the compounds were evaluated for their cytotoxic activity against MCF7, A549, HeLa, and HEK293 cell lines by real time cell analyzer. Etoposide was used as a standard compound. Briefly, ortho substitutions gave better results compared to meta and para substitutions on the N-phenyl ring and compounds bearing ortho substitutions were more effective on MCF7 cell lines than A549 and HeLa cell lines. 2-(2,3- Dioxo-2,3-dihydro-1H -indol-1-yl)-N-(2- isopropylphenyl)acetamide was the most active compound against all the tested cell lines. © TÜBITAK.
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    The synthesis and structural characterization of some 2(3H)-benzoxazolone derivatives
    (2001) Tarikogullari A.H.; Zincircioglu O.
    In this study, five N-phenyl-2-(2-oxobenzoxazoline-3-yl)acetamide derivatives bearing substituents with different lipophilic and electronic properties on N-phenyl ring, beside the nonsubstituted one, have been synthesized. Their structural characterization has been performed by spectral analyses such as IR, 1H NMR and CIMS. 1H NMR data clearly indicated that the title compounds in DMSO-d6 present as a mixture of two different rotamers.
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    Synthesis, biological evaluation and molecular docking study of hydrazone-containing pyridinium salts as cholinesterase inhibitors
    (Pharmaceutical Society of Japan, 2016) Parlar S.; Bayraktar G.; Tarikogullari A.H.; Alptüzün V.; Erciyas E.
    A series of pyridinium salts bearing alkylphenyl groups at 1 position and hydrazone structure at 4 position of the pyridinium ring were synthesized and evaluated for the inhibition of both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) enzymes. The cholinesterase (ChE) inhibitory activity studies were carried out by using the Ellman's colorimetric method. All compounds displayed considerable AChE and BuChE inhibitory activity and some of the compounds manifested remarkable anti-AChE activity compared to the reference compound, galantamine. Among the title compounds, the series including benzofuran aromatic ring exhibited the best inhibitory activity both on AChE and BuChE enzymes. Compound 3b, 4-[2-(1-(benzofuran-2-yl)ethylidene)hydrazinyl]-1-(3-phenylpropyl)pyridinium bromide, was the most active compound with IC50 value of 0.23 (0.24) µM against enantiomeric excess (ee)AChE (human (h)AChE) while compound 3a, 4-[2-(1-(benzofuran-2-yl)ethylidene)hydrazinyl]-1-phenethylpyridinium bromide, was the most active compound with IC50 value of 0.95 µM against BuChE. Moreover, 3a and b exhibited higher activity than the reference compound galantamine (eeAChE (hAChE) IC50 0.43 (0.52) µM; BuChE IC50 14.92 µM). Molecular docking studies were carried out on 3b having highest inhibitory activity against AChE. © 2016 The Pharmaceutical Society of Japan.