| Title : Drug Design of Inhibitors of Alzheimer's Disease (AD): POM and DFT Analyses of Cholinesterase Inhibitory Activity of beta-amino di-Carbonyl Derivatives - Hadda_2019_Mini.Rev.Med.Chem_19_688 |
| Author(s) : Hadda TB , Rauf A , Zgou H , Senol FS , Orhan IE , Mabkhot YN , Althagafi, II , Farghaly TA , Alterary S |
| Ref : Mini Rev Med Chem , 19 :688 , 2019 |
|
Abstract :
BACKGROUND: Since deficit of acetylcholine has been evidenced in the Alzheimer's disease (AD) patients, cholinesterase inhibitors are currently the most specified drug category for the remediation of AD. METHOD: In the present study, 16 compounds (1-16) with dicarbonyl skeletons have been synthesized and tested for their inhibitory potential in vitro against AChE and BChE using ELISA microtiter plate assays at 100 mug/mL. Since metal accumulation is related to AD, the compounds were also tested for their metal-chelation capacity. RESULTS AND CONCLUSION: All the investigated dicarbonyl compounds exerted none or lower than 30% inhibition against both cholinesterases, whereas compounds 2, 8 and 11 showed 37, 42, 41% of inhibition towards BChE, being the most active. The highest metal-chelation capacity was observed with compound 8 (53.58 +/- 2.06%). POM and DFT analyses are in good harmonization with experimental data. |
| PubMedSearch : Hadda_2019_Mini.Rev.Med.Chem_19_688 |
| PubMedID: 30387392 |
Hadda TB, Rauf A, Zgou H, Senol FS, Orhan IE, Mabkhot YN, Althagafi, II, Farghaly TA, Alterary S (2019)
Drug Design of Inhibitors of Alzheimer's Disease (AD): POM and DFT Analyses of Cholinesterase Inhibitory Activity of beta-amino di-Carbonyl Derivatives
Mini Rev Med Chem
19 :688
Hadda TB, Rauf A, Zgou H, Senol FS, Orhan IE, Mabkhot YN, Althagafi, II, Farghaly TA, Alterary S (2019)
Mini Rev Med Chem
19 :688