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  • Küçük Resim
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    Antioxidant, acetylcholinesterase and butyrylcholinesterase inhibition profiles of histamine schiff bases
    (Turkish Chemical Society, 2019) Akocak, Süleyman; Lolak, Nabih; Tuneğ, Muhammed; Boǧa, Mehmet
    In this work, a series of histamine Schiff bases H(1-20) were assayed for antioxidant properties by using different bioanalytical methods such as DPPH-free radical scavenging assay, ABTS cation radical decolarization, cupric reducing antioxidant capacity (CUPRAC) and metal chelating methods. The acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition profiles were also assessed. In general, the synthesized compounds showed weak antioxidant activity against all tested methods, but some of them showed great inhibition potency against AChE and BChE enzymes. Specifically, compound H9 showed effective inhibition potency against both enzymes with percent inhibition of 97.03 and 93.64, respectively.
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    Design, synthesis and biological evaluation of 1,3-diaryltriazene-substituted sulfonamides as antioxidant, acetylcholinesterase and butyrylcholinesterase inhibitors
    (Turkish Chemical Society, 2019) Akocak, Süleyman; Boğa, Mehmet; Lolak, Nabih; Tuneğ, Muhammed; Sanku, Rajesh Kishore Kumar
    1,3-diaryltriazenes are one of the most useful and important linkers for many pharmaceutical applications. Therefore, in the current work, a series of 1,3-diaryltriazene sulfonamides 4(a-k) were synthesized by reacting diazonium salt of sulfanilamide and substituted aromatic amine derivatives 3(a-k). The obtained compounds were investigated for antioxidant properties by using different methods such as a DPPH radical scavenging assay, ABTS radical decolarization, cupric reducing antioxidant capacity (CUPRAC) and metal chelating methods. The cholinesterase inhibition activities (acetylcholinesterase and butyrylcholinesterase) of synthesized compounds were also tested. In general, compounds showed weak antioxidant activity, except compounds 4d (IC50 =114.89 for DPPH activity), 4i (IC50 =25.31 for ABTS activity), 4a (IC50 = 86.33 for metal chelating activity), and 4k (absorbance value 1.229 µM for CUPRAC). Some of the compounds showed great % inhibition against both acetylcholinesterase and butyrylcholinesterase with % inhibition values ranging from 11.54 to 93.67 and 62.24 to 98.47, respectively.
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    Sulphonamides incorporating 1,3,5-triazine structural motifs show antioxidant, acetylcholinesterase, butyrylcholinesterase, and tyrosinase inhibitory profile
    (Taylor and Francis Ltd, 2020) Lolak, Nabih; Boǧa, Mehmet; Tuneğ, Muhammed; Karakoç, Gulçin; Akocak, Suleyman; Supuran, Claudiu T.
    A series of 16 novel benzenesulfonamides incorporating 1,3,5-triazine moieties substituted with aromatic amines, dimethylamine, morpholine and piperidine were investigated. These compounds were assayed for antioxidant properties by using 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assay, 2,2`-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS) radical decolarisation assay and metal chelating methods. They were also investigated as inhibitors of acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and tyrosinase, which are associated with several diseases such as Alzheimer, Parkinson and pigmentation disorders. These benzenesulfonamides showed moderate DPPH radical scavenging and metal chelating activity, and low ABTS cation radical scavenging activity. Compounds 2 b, 3d and 3 h showed inhibitory potency against AChE with % inhibition values of >90. BChE was also effectively inhibited by most of the synthesised compounds with >90% inhibition potency. Tyrosinase was less inhibited by these compounds.