Fluoropezil
AChe IC50 = 2.4 nM. 24r is a mixed-type inhibitor against AChE Ki value equal to 0.4 nM. 24r reduced tau phosphorylation at S396 and Abeta aggregation in the presence of AChE
General
Type : Multitarget, Derivative of Donepezil, Sulfur Compound, Antioxidant, Thiophen
Chemical_Nomenclature : 2-Fluoro-2-((1-(3-fluorobenzyl)piperidin-4-yl)methyl)-5,6-dimethoxy-2,3-dihydrobenzo[b]thiophene 1,1-dioxide || 2-fluoro-2-[[1-[(3-fluorophenyl)methyl]piperidin-4-yl]methyl]-5,6-dimethoxy-3H-1-benzothiophene 1,1-dioxide
Canonical SMILES : C1=CC(=CC(=C1)CN2CCC(CC2)CC4(CC3=CC(=C(C=C3[S]4(=O)=O)OC)OC)F)F || COC1=C(C=C2C(=C1)CC(S2(=O)=O)(CC3CCN(CC3)CC4=CC(=CC=C4)F)F)OC
InChI : InChI=1S\/C23H27F2NO4S\/c1-29-20-11-18-14-23(25,31(27,28)22(18)12-21(20)30-2)13-16-6-8-26(9-7-16)15-17-4-3-5-19(24)10-17\/h3-5,10-12,16H,6-9,13-15H2,1-2H3
InChIKey : IVJYMZOWJKEUNR-UHFFFAOYSA-N
Other name(s) : Donepezil-sulfone-analogue-24r || AChE-IN-10 || 24r || Donepezil sulfone analogue 24r || DC20 || DC511020 || HY-144775 || CS-0434465
MW : 451.52
Formula : C23H27F2NO4S
CAS_number :
PubChem : 163409065
UniChem : IVJYMZOWJKEUNR-UHFFFAOYSA-N
Target
Families : Fluoropezil ligand of proteins in family
ACHE
Protein :
human-ACHE
References (4)
| Title : Novel inhibitors of AChE and Abeta aggregation with neuroprotective properties as lead compounds for the treatment of Alzheimer's disease - Liu_2022_Eur.J.Med.Chem_235_114305 |
| Author(s) : Liu Y , Uras G , Onuwaje I , Li W , Yao H , Xu S , Li X , Phillips J , Allen S , Gong Q , Zhang H , Zhu Z , Liu J , Xu J |
| Ref : Eur Journal of Medicinal Chemistry , 235 :114305 , 2022 |
| Abstract : |
| PubMedSearch : Liu_2022_Eur.J.Med.Chem_235_114305 |
| PubMedID: 35339839 |
| Title : LC-MS\/MS assay of fluoropezil and its two major metabolites in human plasma: an application to pharmacokinetic studies - Guo_2022_Bioanalysis_14_817 |
| Author(s) : Guo R , Hu J , Jing J , Liu Y , Li J , Zhou Y , Liu H , Zhou L , Chen X |
| Ref : Bioanalysis , 14 :817 , 2022 |
| Abstract : |
| PubMedSearch : Guo_2022_Bioanalysis_14_817 |
| PubMedID: 35735138 |
| Title : Safety, tolerability, and pharmacokinetics of fluoropezil (DC20), a novel AChE inhibitor: a singlecenter, phase I study in healthy young and elderly Chinese subjects - Qian_2022_ResearchSquare__ |
| Author(s) : Qian H , Yu C , Zhu H , Ding Q , Cai Y , Jing J , Xu X , Guo R , Zhang H , Liu H , Chen X , Liu Y |
| Ref : ResearchSquare , : , 2022 |
| Abstract : |
| PubMedSearch : Qian_2022_ResearchSquare__ |
| PubMedID: |
| Title : Desorption electrospray ionization (DESI) source coupling ion mobility mass spectrometry for imaging fluoropezil (DC20) distribution in rat brain - Guo_2021_Anal.Bioanal.Chem_413_5835 |
| Author(s) : Guo R , Zhou L , Chen X |
| Ref : Anal Bioanal Chem , 413 :5835 , 2021 |
| Abstract : |
| PubMedSearch : Guo_2021_Anal.Bioanal.Chem_413_5835 |
| PubMedID: 34405263 |