Literature DB >> 31838895

Multifunctional hybrid sulfonamides as novel therapeutic agents for Alzheimer's disease.

Rayala Swetha1, Devendra Kumar1, Sukesh K Gupta1, Ankit Ganeshpurkar1, Ravi Singh1, Gopichand Gutti1, Dileep Kumar1, Srabanti Jana1, Sairam Krishnamurthy1, Sushil K Singh1.   

Abstract

Aim: A breakthrough in modern medicine, in terms of treatment of Alzheimer's disease, is yet to be seen, as the scene is currently plagued with numerous clinical trial failures. Here, we are exploring multifunctional hybrid sulfonamides for their anti-Alzheimer activity due to the complex nature of the disease. Results & methodology: Compound 41 showed significant inhibition of MMP-2 (IC50: 18.24 ± 1.62 nM), AChE (IC50: 4.28 ± 0.15 μM) and BuChE (IC50: 1.32 ± 0.02 μM). It also exhibited a metal-chelating property, as validated by an in vitro metal-induced Aβ aggregation assay using confocal fluorescence imaging. Whereas, MTT and DPPH assays revealed it to be nontoxic and neuroprotective with substantial antioxidant property.
Conclusion: The present study puts forth potent yet nontoxic lead molecules, which foray into the field of multitargeted agents for the treatment of Alzheimer's disease.

Entities:  

Keywords:  Alzheimer’s disease; acetylcholine esterase; amyloid β; butyrylcholinesterase; confocal fluorescence microscopy; matrix metalloproteinase-2; metal chelation; β-alanine

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Year:  2019        PMID: 31838895     DOI: 10.4155/fmc-2019-0106

Source DB:  PubMed          Journal:  Future Med Chem        ISSN: 1756-8919            Impact factor:   3.808


  2 in total

1.  Improved machine learning scoring functions for identification of Electrophorus electricus's acetylcholinesterase inhibitors.

Authors:  Ankit Ganeshpurkar; Ravi Singh; Shalini Shivhare; Devendra Kumar; Gopichand Gutti; Ravibhushan Singh; Ashok Kumar; Sushil Kumar Singh
Journal:  Mol Divers       Date:  2021-07-30       Impact factor: 2.943

2.  New Hybrids of 4-Amino-2,3-polymethylene-quinoline and p-Tolylsulfonamide as Dual Inhibitors of Acetyl- and Butyrylcholinesterase and Potential Multifunctional Agents for Alzheimer's Disease Treatment.

Authors:  Galina F Makhaeva; Nadezhda V Kovaleva; Natalia P Boltneva; Sofya V Lushchekina; Tatiana Yu Astakhova; Elena V Rudakova; Alexey N Proshin; Igor V Serkov; Eugene V Radchenko; Vladimir A Palyulin; Sergey O Bachurin; Rudy J Richardson
Journal:  Molecules       Date:  2020-08-27       Impact factor: 4.411

  2 in total

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