Design, Synthesis, Biological Evaluation, and Docking Study of Acetylcholinesterase Inhibitors: New Acridone-1,2,4-Oxadiazole-1,2,3-Triazole Hybrids

Science Communicator Platform

Stay connected! Follow us on X network (Twitter):

Share By

Design, Synthesis, Biological Evaluation, and Docking Study of Acetylcholinesterase Inhibitors: New Acridone-1,2,4-Oxadiazole-1,2,3-Triazole Hybrids Publisher Pubmed

Mohammadikhanaposhtani M¹ ; Mahdavi M² ; Saeedi M³ ; Sabourian R⁴ ; Safavi M⁵ ; Khanavi M⁶ ; Foroumadi A² ; Shafiee A² ; Akbarzadeh T^{1, 4}

Source: Chemical Biology and Drug Design Published:2015

Abstract

In this study, novel acridone-1,2,4-oxadiazole-1,2,3-triazole hybrids were designed, synthesized, and evaluated for their acetylcholinesterase and butyrylcholinesterase inhibitory activity. Among various synthesized compounds, 10-((1-((3-(4-methoxyphenyl)-1,2,4-oxadiazol-5-yl)methyl)-1H-1,2,3-triazol-4-yl)methyl)acridin-9(10H)-one 10b showed the most potent anti-acetylcholinesterase activity (IC50 = 11.55 μm) being as potent as rivastigmine. Also docking outcomes were in good agreement with in vitro results confirming the dual binding inhibitory activity of compound 10b. A novel series of acridone-1,2,4-oxadiazole-1,2,3-triazole hybrids were synthesized and evaluated in vitro for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities. © 2015 John Wiley & Sons A/S.

Related Docs

View other Related Docs

1. Potent Acetylcholinesterase Inhibitors: Design, Synthesis, Biological Evaluation, and Docking Study of Acridone Linked to 1,2,3-Triazole Derivatives, European Journal of Medicinal Chemistry (2015)

2. Novel Tacrine-1,2,3-Triazole Hybrids: In Vitro, in Vivo Biological Evaluation and Docking Study of Cholinesterase Inhibitors, European Journal of Medicinal Chemistry (2017)

3. A Review on Tacrine-Based Scaffolds As Multi-Target Drugs (Mtdls) for Alzheimer's Disease, European Journal of Medicinal Chemistry (2017)

Experts (# of related papers)

View all Related Experts

Mohammad Mahdavi (15)

Alireza Foroumadi (12)

Other Related Docs

4. Design, Synthesis, Molecular Modeling and Anticholinesterase Activity of Benzylidene-Benzofuran-3-Ones Containing Cyclic Amine Side Chain, Future Medicinal Chemistry (2017)

5. Design, Synthesis, Pharmacological Evaluation, and Docking Study of New Acridone-Based 1,2,4-Oxadiazoles As Potential Anticonvulsant Agents, European Journal of Medicinal Chemistry (2016)

6. Synthesis of Novel 1,2,3-Triazole-Dihydro[3,2-C[Chromenones As Acetylcholinesterase Inhibitors, Synthetic Communications (2015)

7. Design and Synthesis of Benzodiazepine-1,2,3-Triazole Hybrid Derivatives As Selective Butyrylcholinesterase Inhibitors, Molecular Diversity (2020)

8. Synthesis and Anticholinergic Activity of 4-Hydroxycoumarin Derivatives Containing Substituted Benzyl-1,2,3-Triazole Moiety, Chemical Biology and Drug Design (2015)

9. Design, Synthesis and Anti-Alzheimer's Activity of Novel 1,2,3-Triazole-Chromenone Carboxamide Derivatives, Bioorganic Chemistry (2019)

10. Design and Synthesis of Novel Anti-Alzheimer's Agents: Acridine-Chromenone and Quinoline-Chromenone Hybrids, Bioorganic Chemistry (2016)

11. Cholinesterase Inhibition Activity and Docking Simulation Study of Coumarin Mannich Base Derivatives, Journal of Sciences# Islamic Republic of Iran (2019)

12. Synthesis of Novel Chromenones Linked to 1,2,3-Triazole Ring System: Investigation of Biological Activities Against Alzheimer's Disease, Bioorganic Chemistry (2017)

13. Coumarin Derivatives Bearing Benzoheterocycle Moiety: Synthesis, Cholinesterase Inhibitory, and Docking Simulation Study, Iranian Journal of Basic Medical Sciences (2017)

14. Design, Synthesis, in Vitro Cytotoxic Activity Evaluation, and Apoptosis-Induction Study of New 9(10H-Acridinone-1,2,3-Triazoles, Molecular Diversity (2015)

15. Anticholinesterase Activity of Cinnamic Acids Derivatives: In Vitro, in Vivo Biological Evaluation, and Docking Study, Letters in Drug Design and Discovery (2020)

16. Synthesis and Antiacetylcholinesterase Activity Evaluation of New 2-Aryl Benzofuran Derivatives, Letters in Drug Design and Discovery (2016)

17. Design, Synthesis, in Vivo and in Vitro Studies of 1,2,3,4-Tetrahydro-9H-Carbazole Derivatives, Highly Selective and Potent Butyrylcholinesterase Inhibitors, Molecular Diversity (2020)

18. Novel Tetrahydrocarbazole Benzyl Pyridine Hybrids As Potent and Selective Butryl Cholinesterase Inhibitors With Neuroprotective and Β-Secretase Inhibition Activities, European Journal of Medicinal Chemistry (2018)

19. Synthesis and Biological Evaluation of New N-Benzylpyridinium-Based Benzoheterocycles As Potential Anti-Alzheimer's Agents, Bioorganic Chemistry (2019)

20. Design and Synthesis of Novel Coumarin-Pyridinium Hybrids: In Vitro Cholinesterase Inhibitory Activity, Bioorganic Chemistry (2018)

Style	Citing Format
MLA	Mohammadikhanaposhtani M, et al.. "Design, Synthesis, Biological Evaluation, and Docking Study of Acetylcholinesterase Inhibitors: New Acridone-1,2,4-Oxadiazole-1,2,3-Triazole Hybrids." Chemical Biology and Drug Design, vol. 86, no. 6, 2015, pp. 1425-1432.
APA	Mohammadikhanaposhtani M, Mahdavi M, Saeedi M, Sabourian R, Safavi M, Khanavi M, Foroumadi A, Shafiee A, Akbarzadeh T (2015). Design, Synthesis, Biological Evaluation, and Docking Study of Acetylcholinesterase Inhibitors: New Acridone-1,2,4-Oxadiazole-1,2,3-Triazole Hybrids. Chemical Biology and Drug Design, 86(6), 1425-1432.
Chicago	Mohammadikhanaposhtani M, Mahdavi M, Saeedi M, Sabourian R, Safavi M, Khanavi M, Foroumadi A, Shafiee A, Akbarzadeh T. "Design, Synthesis, Biological Evaluation, and Docking Study of Acetylcholinesterase Inhibitors: New Acridone-1,2,4-Oxadiazole-1,2,3-Triazole Hybrids." Chemical Biology and Drug Design 86, no. 6 (2015): 1425-1432.
Harvard	Mohammadikhanaposhtani M et al. (2015) 'Design, Synthesis, Biological Evaluation, and Docking Study of Acetylcholinesterase Inhibitors: New Acridone-1,2,4-Oxadiazole-1,2,3-Triazole Hybrids', Chemical Biology and Drug Design, 86(6), pp. 1425-1432.
Vancouver	Mohammadikhanaposhtani M, Mahdavi M, Saeedi M, Sabourian R, Safavi M, Khanavi M, et al.. Design, Synthesis, Biological Evaluation, and Docking Study of Acetylcholinesterase Inhibitors: New Acridone-1,2,4-Oxadiazole-1,2,3-Triazole Hybrids. Chemical Biology and Drug Design. 2015;86(6):1425-1432.
BibTex	@article{ author = {Mohammadikhanaposhtani M and Mahdavi M and Saeedi M and Sabourian R and Safavi M and Khanavi M and Foroumadi A and Shafiee A and Akbarzadeh T}, title = {Design, Synthesis, Biological Evaluation, and Docking Study of Acetylcholinesterase Inhibitors: New Acridone-1,2,4-Oxadiazole-1,2,3-Triazole Hybrids}, journal = {Chemical Biology and Drug Design}, volume = {86}, number = {6}, pages = {1425-1432}, year = {2015} }
RIS	TY - JOUR AU - Mohammadikhanaposhtani M AU - Mahdavi M AU - Saeedi M AU - Sabourian R AU - Safavi M AU - Khanavi M AU - Foroumadi A AU - Shafiee A AU - Akbarzadeh T TI - Design, Synthesis, Biological Evaluation, and Docking Study of Acetylcholinesterase Inhibitors: New Acridone-1,2,4-Oxadiazole-1,2,3-Triazole Hybrids JO - Chemical Biology and Drug Design VL - 86 IS - 6 SP - 1425 EP - 1432 PY - 2015 ER -

Science Communicator Platform

Authors

Abstract