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Research Article

Enzyme inhibitory potential of some indole Schiff bases on acetylcholinesterase and human carbonic anhydrase isoforms I and II enzymes: an in vitro and molecular docking study

, ORCID Icon, , ORCID Icon &
Received 11 Jul 2023, Accepted 27 Sep 2023, Published online: 20 Oct 2023
 

Abstract

In this study, the in vitro effects of some indole Schiff bases on acetylcholinesterase and human carbonic anhydrase isoforms I and II were investigated. A series of N-methylindole hydrazide/hydrazone derivatives (1a-1t) were tested on these enzymes. The interactions of the synthesized indole derivatives with target enzymes were studied by molecular docking methodology. The results revealed that indole derivative Schiff base compounds inhibited the enzymes significantly. Ki values for hCAI isoenzyme were determined to be in the range of 36.18 ± 3.07–224.29 ± 5.78 nM; for the hCAII isoenzyme in the range of 31.30 ± 2.63–201.64 ± 7.25 nM; for acetylcholinesterase in the range of 6.82 ± 0.72–110.30 ± 9.26 nM. Compared to the control compound Acetazolamide (AZA), 1k and 1p were found to have the best inhibitory effect for hCAI; 1p was found to be the best inhibitory effect for hCAII. Compared to the control compound Tacrine (TAC), 1s showed the best inhibitory effect for AChE. In vitro results were verified with the results obtained by docking studies and interactions with enzymes were demonstrated.

Communicated by Ramaswamy H. Sarma

Author contribution statement

Sirinzade H and Dilek E. written manuscript; Dilek E. and Suzen S. designed the study, prepared protocols, analyzed the data; Dilek E., Akman E., Shirinzadeh H. and Ozguven-Yilmaz S.; performed the experiments and participated in discussions. All the authors were responsible for the data acquisition, review and editing of the manuscript.

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This work was supported by the Scientific Research Council of Erzincan Binali Yildirim University (Project No: TSA-2020-663).

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