An article 4,6-Diphenylpyrimidine Derivatives as Dual Inhibitors of Monoamine Oxidase and Acetylcholinesterase for the Treatment of Alzheimer’s Disease WOS:000456351300032 published article about BIOLOGICAL EVALUATION; FUTURE TREATMENTS; DIRECTED LIGANDS; CELL MODEL; DONEPEZIL; MAO; CHOLINESTERASE; SYMPTOMS; HYBRIDS; DESIGN in [Kumar, Bhupinder; Dwivedi, Ashish Ranjan; Kumar, Vinod] Cent Univ Punjab, Dept Pharmaceut Sci & Nat Prod, Lab Organ & Med Chem, Bathinda 151001, Punjab, India; [Sarkar, Bibekananda; Mantha, Anil K.; Parkash, Jyoti] Cent Univ Punjab, Sch Basic & Appl Sci, Dept Anim Sci, Bathinda 151001, Punjab, India; [Gupta, Sukesh Kumar; Krishnamurthy, Sairam] Banaras Hindu Univ, Indian Inst Technol, Dept Pharmaceut Engn & Technol, Varanasi 221005, Uttar Pradesh, India in 2019.0, Cited 46.0. Quality Control of 4′-Hydroxyacetophenone. The Name is 4′-Hydroxyacetophenone. Through research, I have a further understanding and discovery of 99-93-4
Alzheimer’s disease (AD) is a neurodegenerative disorder with multifactorial pathogenesis. Monoamine oxidase (MAO) and acetylcholinesterase enzymes (AChE) are potential targets for the treatment of AD. A total of 15 new propargyl containing 4,6-diphenylpyrimidine derivatives were synthesized and screened for the MAO and AChE inhibition activities along with ROS production inhibition and metal-chelation potential. All the synthesized compounds were found to be selective and potent inhibitors of MAO-A and AChE enzymes at nanomolar concentrations. VB1 was found to be the most potent MAO-A and BuChE inhibitor with IC50 values of 18.34 +/- 0.38 nM and 0.666 +/- 0.03 mu M, respectively. It also showed potent AChE inhibition with an IC50 value of 30.46 +/- 0.23 nM. Compound VB8 was found to be the most potent AChE inhibitor with an IC50 value of 9.54 +/- 0.07 nM and displayed an IC50 value of 1010 +/- 70.42 nM against the MAO-A isoform. In the cytotoxic studies, these compounds were found to be nontoxic to the human neuroblastoma SH-SYSY cells even at 25 mu M concentration. All the compounds were found to be reversible inhibitors of MAO-A and AChE enzymes. In addition, these compounds also showed good neuroprotective properties against 6-OHDA- and H2O2-induced neurotoxicity in SH-SYSY cells. All the compounds accommodate nicely to the hydrophobic cavity of MAO-A and AChE enzymes. In the molecular dynamics simulation studies, both VB1 and VB8 were found to be stable in the respective cavities for 30 ns. Thus, 4,6-diphenylpyrimidine derivatives can act as promising leads in the development of dual-acting inhibitors targeting MAO-A and AChE enzymes for the treatment of Alzheimer’s disease.
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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles