Literature DB >> 26077890

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

Maryam Mohammadi-Khanaposhtani1, Mohammad Mahdavi2, Mina Saeedi3,4, Reyhaneh Sabourian4, Maliheh Safavi5, Mahnaz Khanavi6, Alireza Foroumadi2, Abbas Shafiee2, Tahmineh Akbarzadeh1,4.   

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.
© 2015 John Wiley & Sons A/S.

Entities:  

Keywords:  Alzheimer's disease; acetylcholinesterase; acridone-1,2,4-oxadiazole-1,2,3-triazole; docking study

Mesh:

Substances:

Year:  2015        PMID: 26077890     DOI: 10.1111/cbdd.12609

Source DB:  PubMed          Journal:  Chem Biol Drug Des        ISSN: 1747-0277            Impact factor:   2.817


  4 in total

Review 1.  Inhibitory potential of nitrogen, oxygen and sulfur containing heterocyclic scaffolds against acetylcholinesterase and butyrylcholinesterase.

Authors:  Rami J Obaid; Nafeesa Naeem; Ehsan Ullah Mughal; Munirah M Al-Rooqi; Amina Sadiq; Rabab S Jassas; Ziad Moussa; Saleh A Ahmed
Journal:  RSC Adv       Date:  2022-07-12       Impact factor: 4.036

2.  Design and synthesis of 4,5-diphenyl-imidazol-1,2,3-triazole hybrids as new anti-diabetic agents: in vitro α-glucosidase inhibition, kinetic and docking studies.

Authors:  Mohammad Sadegh Asgari; Maryam Mohammadi-Khanaposhtani; Zeinab Sharafi; Mohammad Ali Faramarzi; Hossein Rastegar; Ensieh Nasli Esfahani; Fatemeh Bandarian; Parviz Ranjbar Rashidi; Rahmatollah Rahimi; Mahmood Biglar; Mohammad Mahdavi; Bagher Larijani
Journal:  Mol Divers       Date:  2020-03-18       Impact factor: 2.943

3.  Design, synthesis, and evaluation of novel cinnamic acid-tryptamine hybrid for inhibition of acetylcholinesterase and butyrylcholinesterase.

Authors:  Shahrzad Ghafary; Roshanak Ghobadian; Mohammad Mahdavi; Hamid Nadri; Alireza Moradi; Tahmineh Akbarzadeh; Zahra Najafi; Mohammad Sharifzadeh; Najmeh Edraki; Farshad Homayouni Moghadam; Mohsen Amini
Journal:  Daru       Date:  2020-05-05       Impact factor: 3.117

Review 4.  Medicinal chemistry of acridine and its analogues.

Authors:  Parteek Prasher; Mousmee Sharma
Journal:  Medchemcomm       Date:  2018-08-14       Impact factor: 3.597

  4 in total

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