Literature DB >> 23988412

Design, synthesis, docking study and biological evaluation of some novel tetrahydrochromeno [3',4':5,6]pyrano[2,3-b]quinolin-6(7H)-one derivatives against acetyl- and butyrylcholinesterase.

Mehdi Khoobi1, Masoumeh Alipour, Alireza Moradi, Amirhossein Sakhteman, Hamid Nadri, Seyyede Faeze Razavi, Mehdi Ghandi, Alireza Foroumadi, Abbas Shafiee.   

Abstract

Novel hybrid derivatives of two known scaffolds; tetrahydroaminoquinoline and coumarin were synthesized and evaluated for both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) activities. By means of an efficient nanocatalyst, the reaction time for the syntheses of the target compounds was reduced. Subsequently, Ellman's modified method was used to evaluate the enzyme inhibitory activity of the synthesized structures. It was observed that most hybrid structures were moderate to potent inhibitors of AChE compared to Tacrine as the reference drug among which 7f with 4-fluorophenyl substituent was the most active compound (IC50=5 nM).
Copyright © 2013 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Alzheimer's disease; Cholinesterase inhibitor; Coumarin; Docking study; Tacrine

Mesh:

Substances:

Year:  2013        PMID: 23988412     DOI: 10.1016/j.ejmech.2013.07.045

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  5 in total

Review 1.  Multi-Target Drug Candidates for Multifactorial Alzheimer's Disease: AChE and NMDAR as Molecular Targets.

Authors:  Md Sahab Uddin; Abdullah Al Mamun; Md Tanvir Kabir; Ghulam Md Ashraf; May N Bin-Jumah; Mohamed M Abdel-Daim
Journal:  Mol Neurobiol       Date:  2020-09-15       Impact factor: 5.590

Review 2.  Profiling donepezil template into multipotent hybrids with antioxidant properties.

Authors:  Eva Mezeiova; Katarina Spilovska; Eugenie Nepovimova; Lukas Gorecki; Ondrej Soukup; Rafael Dolezal; David Malinak; Jana Janockova; Daniel Jun; Kamil Kuca; Jan Korabecny
Journal:  J Enzyme Inhib Med Chem       Date:  2018-12       Impact factor: 5.051

Review 3.  Molecular docking studies of coumarin hybrids as potential acetylcholinesterase, butyrylcholinesterase, monoamine oxidase A/B and β-amyloid inhibitors for Alzheimer's disease.

Authors:  Samina Khan Yusufzai; Mohammad Shaheen Khan; Othman Sulaiman; Hasnah Osman; Dalily Nabilah Lamjin
Journal:  Chem Cent J       Date:  2018-12-04       Impact factor: 4.215

4.  Cysteic acid grafted to magnetic graphene oxide as a promising recoverable solid acid catalyst for the synthesis of diverse 4H-chromene.

Authors:  Firouz Matloubi Moghaddam; Mohammad Eslami; Golfamsadat Hoda
Journal:  Sci Rep       Date:  2020-12-01       Impact factor: 4.379

5.  Cholinesterase inhibitory activity of tinosporide and 8-hydroxytinosporide isolated from Tinospora cordifolia: In vitro and in silico studies targeting management of Alzheimer's disease.

Authors:  Mohiminul Adib; Rashedul Islam; Monira Ahsan; Arifur Rahman; Mahmud Hossain; Md Mustafizur Rahman; Sultan M Alshehri; Mohsin Kazi; Md Abdul Mazid
Journal:  Saudi J Biol Sci       Date:  2021-03-30       Impact factor: 4.219

  5 in total

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