Abstract:
:The synthesis of racemic tetrahydrocurcumin- (THC-), tetrahydrodemethoxycurcumin- (THDC-) and tetrahydrobisdemethoxycurcumin- (THBDC-) dihydropyrimidinone (DHPM) analogues was achieved by utilizing the multi-component Biginelli reaction in the presence of copper sulphate as a catalyst. The evaluation of acetylcholinesterase inhibitors for Alzheimer's disease of these compounds showed that they exhibited higher inhibitory activity than their parent analogues. THBDC-DHPM demonstrated the most potent inhibitory activity with an IC50 value of 1.34±0.03μM which was more active than the approved drug galanthamine (IC50=1.45±0.04μM).
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Arunkhamkaew S,Athipornchai A,Apiratikul N,Suksamrarn A,Ajavakom Vdoi
10.1016/j.bmcl.2013.03.069subject
Has Abstractpub_date
2013-05-15 00:00:00pages
2880-2issue
10eissn
0960-894Xissn
1464-3405pii
S0960-894X(13)00397-1journal_volume
23pub_type
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