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    In Silico studies and DNA cleavage, antioxidant, acetylcholinesterase, and butyrylcholinesterase activity evaluation of bis-histamine schiff bases and bis-spinaceamine substituted derivatives
    (Springer, 2022) Lolak, Nebih; Boğa, Mehmet; Sönmez, Görkem Deniz; Tuneğ, Muhammed; Doğan, Aslınur; Akocak, Süleyman
    In this work, a series of seven bis-histamine Schiff bases (H1-H4) and bis-spinaceamine substituted derivatives (SPH1, SPH2, and SPH4) were successfully re-synthesized to evaluate their antioxidant properties by several bioanalytical methods such as DPPH free radical scavenging assay, ABTS radical cation decolorization assay, metal chelating and CUPRAC methods. On the other hand, these compounds were also investigated as inhibitors of acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and DNAcleavage. The results revealed that all compounds showed, in general, moderate DPPH and ABTS radical scavenging activities, and low metal chelating and CUPRAC activities. Specifically, compound SPH4 showed good DPPH radical scavenging activity with IC50 value of 59.59 mu M, which is better than the BHA and BHT standard values. The best AChE and BChE inhibition results among the tested series were also obtained for compound SPH4 with % inhibition values of 84.51 and 75.89, respectively. Taken together, compound SPH4 might be an interesting lead compound to discover more potent agents against these enzymes.
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    Synthesis of calix[4]azacrown substituted sulphonamides with antioxidant, acetylcholinesterase, butyrylcholinesterase, tyrosinase and carbonic anhydrase inhibitory action
    (Taylor and Francis Ltd., 2020) Oğuz, Mehmet; Kalay, Erbay; Akocak, Süleyman; Nocentini, Alessio; Lolak, Nebih; Boğa, Mehmet; Yılmaz, Mustafa; Supuran, Claudiu T.
    A series of novel calix[4]azacrown substituted sulphonamide Schiff bases was synthesised by the reaction of calix[4]azacrown aldehydes with different substituted primary and secondary sulphonamides. The obtained novel compounds were investigated as inhibitors of six human (h) isoforms of carbonic anhydrases (CA, EC 4.2.1.1). Their antioxidant profile was assayed by various bioanalytical methods. The calix[4]azacrown substituted sulphonamide Schiff bases were also investigated as inhibitors of acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and tyrosinase enzymes, associated with several diseases such as Alzheimer, Parkinson, and pigmentation disorders. The new sulphonamides showed low to moderate inhibition against hCAs, AChE, BChE, and tyrosinase enzymes. However, some of them possessed relevant antioxidant activity, comparable with standard antioxidants used in the study.