Acetylcholinesterase and Butyrylcholinesterase Inhibitory Activities of 5-Arylidene-N, N-Diethylthiobarbiturates | [Journal of Chemical Society of Pakistan • 2020]

Author(s):

1. Momin Khan: Department of Chemistry, Abdul Wali Khan University, Mardan, Pakistan

2. Munir Ur Rehman: Department of Chemistry, Abdul Wali Khan University, Mardan, Pakistan

3. Naveed Qadir: Department of Chemistry, Abdul Wali Khan University, Mardan, Pakistan

4. Muhammad Ashraf: Department of Biochemistry and Biotechnology, The Islamia University of Bahawalpur, Bahawalpur-63100. Pakistan

5. Tayaba Ismail: Department of Biochemistry and Biotechnology, The Islamia University of Bahawalpur, Bahawalpur-63100. Pakistan

6. Muhammad Ismail: Department of Chemistry, Abdul Wali Khan University, Mardan-23200, Pakistan

7. Kanwal: H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan

8. Uzma Salar: Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan

9. Khalid Mohammed Khan: H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan; Department of Clinical Pharmacy, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, Dammam Saudi Arabia.

10. Shahnaz Perveen: PCSIR Laboratoires Complex, Karachi, Shahrah-e-Dr. Salimuzzaman Siddiqui, Karachi, Pakistan

Abstract:

Summary: 5-Arylidene-N,N-diethylthiobarbiturates 1-25 were evaluated for their potential against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes and displayed varying degree of inhibition. Based on the IC50 values, compound 6 (IC50 = 92.51 ± 0.01 µM) was the only active compound against acetylcholinesterase, however this compound was also weakly active against butyrylcholinesterase with an IC50 value 124.76 ± 0.02 µM. Six compounds 1, 6, 7, 16, 17, and 18 showed weak inhibition against BChE, among them compound 18 (IC50 = 82.25 ± 0.07µM) showed good inhibition against BChE. Nevertheless, compounds 1, 7, 16, 17, and 18 were selectively active against BChE enzyme.

Page(s): 134-140

DOI: DOI not available

Published: Journal: Journal of Chemical Society of Pakistan, Volume: 42, Issue: 1, Year: 2020

Keywords:

in vitro , enzyme inhibition , butyrylcholinesterase , NDiethylthiobarbiturates , Acetylcholinesterase , Eserine

References:

References are not available for this document.

Citations

Citations are not available for this document.

Citations

Downloads

Views