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TOK, FATİH

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FATİH

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    Novel 2,5-disubstituted-1,3,4-oxadiazole derivatives as MAO-B inhibitors: Synthesis, biological evaluation and molecular modeling studies
    (ACADEMIC PRESS INC ELSEVIER SCIENCE, 2021) KAYMAKÇIOĞLU, BEDİA; Tok, Fatih; Ugras, Zefine; Saglik, Begum Nurpelin; Ozkay, Yusuf; Kaplancikli, Zafer Asim; Kocyigit-Kaymakcioglu, Bedia
    Thirty novel 2,5-disubstituted-1,3,4-oxadiazole derivatives bearing urea moiety were designed and synthesized. IR, 1H-NMR, 13C-NMR and mass spectroscopic methods and elemental analysis were used to confirm the structures of the compounds. Their monoamine oxidase inhibitory activity was determined against the MAO-A and MAO-B isoforms. None of the compounds showed the potent MAO-A inhibitory activity, while the MAO-B inhibition was significantly found in the range of 62 to 98%. Among them, the compounds H8, H9 and H12 bearing chloro substituent at the fourth position of phenylurea were found to show potent monoamine oxidase B inhibitory activity with IC50 values 0.039-0.066 mu M. To define and evaluate the interaction mechanism between compound H8 and monoamine oxidase B, molecular docking studies have been made.
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    A new series of 1,3,4-oxadiazole derivatives: Synthesis and evaluation of antimicrobial activity
    (2021-11-12) TOK, FATİH; TOK F., ÖZARDA M. G.
    Aim: Infectious diseases have become more and more life-threatening illnesses. Despite a large number of antimicrobial agents, deaths due to infectious diseases are increasing day by day. Antimicrobial drugs have remained insufficiently against some infectious diseases caused outbreaks such as Zika, Ebola, SARS and MERS coronaviruses during the last decades. Therefore, new antimicrobial agents are urgently needed. 1,3,4-Oxadiazole ring is an important pharmacophoric group which is exhibited a broad spectrum of pharmacological activity profile including their antibacterial, antifungal, antiviral, antimalarial, antitubercular properties (1). In this study, we aimed the synthesis of new 1,3,4-oxadiazole rings and evaluation of their antimicrobial activity. Methods: New 2,5-disubstituted-1,3,4-oxadiazoles were synthesized at three steps. All compounds were characterized with spectral methods such as IR, 1H-NMR, 13C-NMR and elemental analysis. The antimicrobial activity of 1,3,4-oxadiazoles was screened on four bacteria and three fungi according to our previous method (2). Enterococcus faecalis, Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus were used for antibacterial activity; Candida albicans, Candida parapsilosis and Candida glabrata were used for anticandidal activity. Results: Minimum inhibitory concentration (MIC) was determined for test compounds and for the reference standards chloramphenicol, ketoconazole. The compound carrying methoxy substituent on the para position of the aromatic ring exhibited the same antibacterial activity as chloramphenicol against E. faecalis with a MIC50 value of 62.50 µM/mL. Conclusions: According to the results, we demonstrated that some compounds exhibit antimicrobial activities against tested microorganisms. Therefore, the oxadiazole nucleus is promising for new drug candidates.