In Silico Studies and DNA Cleavage, Antioxidant, Acetylcholinesterase, and Butyrylcholinesterase Activity Evaluation of Bis-Histamine Schiff Bases and Bis-Spinaceamine Substituted Derivatives

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 rad...

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Bibliographic Details
Published in:Pharmaceutical chemistry journal 2022-03, Vol.55 (12), p.1338-1344
Main Authors: Lolak, Nebih, Boga, Mehmet, Sonmez, Gorkem Deniz, Tuneg, Muhammed, Dogan, Aslinur, Akocak, Suleyman
Format: Article
Language:English
Subjects:
Analysis
Antioxidants
DNA
Ethylenediaminetetraacetic acid
Genetic research
Histamine
Medicine
Organic Chemistry
Pharmacology/Toxicology
Pharmacy
Schiff bases
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Summary: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 IC 50 value of 59.59 μM, 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.
ISSN:0091-150X
1573-9031
DOI:10.1007/s11094-022-02581-7