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2-Mercaptobenzimidazole Derivatives as Novel Butyrylcholinesterase Inhibitors: Biology-Oriented Drug Synthesis (BIODS), In-Vitro and In-Silico Evaluation
Author(s)
Muhammad Yousaf Department of Chemistry, Abdul Wali Khan University,Mardan- 23200,Pakistan
Momin Khan Department of Chemistry, University of Malakand,P.O. Box 18800, Dir Lower Khyber Pakhtunkhwa, Pakistan
Mumtaz Ali 2Department of Chemistry, University of Malakand, P.O. Box 18800, Dir Lower Khyber Pakhtunkhwa, Pakistan.
Abdul Wadood Department of Biochemistry, Abdul Wali Khan University,Mardan- 23200, Pakistan
Ashfaq Ur Rehman Department of Biochemistry, Abdul Wali Khan University, Mardan- 23200, Pakistan
Muhammad Saeed Jan Department of Pharmacy, University of Malakand, P.O. Box 18800, Dir Lower, Khyber Pakhtunkhwa, Pakistan.
Abdul Sadiq Department of Pharmacy, University of Malakand, P.O. Box 18800, Dir Lower, Khyber Pakhtunkhwa, Pakistan.
Faima Alam Department of Biochemistry, Abdul Wali Khan University,Mardan- 23200, Pakistan
Abstract
Summary: Schiff bases gaining remarkable importance day by day in the current situation Schiff bases are found to be a valuable pharmacophore for the synthesis and development of various biologically active heterocyclic compounds. In recent past, we have reported various classes of compounds as enzyme inhibitors, in continuation; A series of 2-Mercaptobenzimidazole hydrazone derivatives (9-42) were synthesized through multistep reactions in high yields and evaluated for butyrylcholinesterase inhibition. In present study, 2-ethylthio benzimidazole was formed by the reaction of 2Mercaptobenzimidazole with bromoethane. In the second step (2-(2-(ethylthio)benzimidazolyl)acetate) obtained by the reaction of 2-ethylthio benzimidazole with ethyl chloroacetate. In the third step, 2-(2(ethylthio)benzimidazolyl)acetate was refluxed in methanol with hydrazine hydrate and get 2((ethylthio)benzimidazolyl)acetohyrazide. In the last step, 2-((ethylthio)benzimidazolyl)acetohyrazide was reacted with different aldehydes in the presence of glacial acetic acid (catalyst) to get a series of 2Mercaptobenzimidazole hydrazone derivatives. Product was characterized by 1H NMR and 13C NMR. These newly synthesized compounds showed varying degree of butyrylcholinesterase inhibition. Compound no. 15 with (IC50 = 25.10 ± 0.90 µM) was found to be most active in the whole series. Similarly, compounds 42, 12, 40, 17, 22, 28 and 09 exhibited excellent activity with IC50 values are (IC50 = 25.36 ± 0.57 µM, IC50 = 27.30 ± 0.52 µM, IC50 = 34.31 ± 0.59 µM, IC50 = 51.29 ± 0.64 µM, IC50 = 54.52 ± 0.95 µM, IC50 = 57.90 ± 0.45 µM and IC50 = 60.93 ±0.67 µM) respectively as compared to standard galantamine 18.13±0.20 µM. Molecular docking helped to find interactions between butyrylcholinesterase enzyme and test compounds. This study results that Schiff bases have been discovered a new class of butyrylcholinesterase inhibitors which have not been discovered earlier.
Publication Details
Page(s) 263-273
DOI DOI not available
Published Journal: Journal of Chemical Society of Pakistan, Volume: 42, Issue: 2, Year: 2020
Keywords
In silico Hydrazone Schiffs bases Benzimidazole2thiol
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