Design, synthesis, and biological activity evaluation of BACE1 inhibitors with antioxidant activity
© 2019 Wiley Periodicals, Inc..
The proteolytic enzyme β-secretase (BACE1) plays a central role in the synthesis of the pathogenic β-amyloid peptides (Aβ) in Alzheimer's disease (AD), antioxidants could attenuate the AD syndrome and prevent the disease progression. In this study, BACE1 inhibitors (D1-D18) with free radical-scavenging activities were synthesized by molecular hybridization of 2-aminopyridine with natural antioxidants. The biological activity evaluation showed that D1 had obvious inhibitory activity against BACE1, and strong antioxidant activity in 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azinobis-(3-ethylbenzthiazoline-6-sulphonate) (ABTS+• ) assay, which could be used as a lead compound for further study.
| Medienart: |
E-Artikel |
|---|
| Erscheinungsjahr: |
2020 |
|---|---|
| Erschienen: |
2020 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:81 |
|---|---|
| Enthalten in: |
Drug development research - 81(2020), 2 vom: 15. Apr., Seite 206-214 |
| Sprache: |
Englisch |
|---|
| Beteiligte Personen: |
Li, He-Min [VerfasserIn] |
|---|
| Links: |
|---|
| Anmerkungen: |
Date Completed 09.07.2021 Date Revised 09.07.2021 published: Print-Electronic Citation Status MEDLINE |
|---|
| doi: |
10.1002/ddr.21585 |
|---|
| funding: |
|
|---|---|
| Förderinstitution / Projekttitel: |
|
| PPN (Katalog-ID): |
NLM300081103 |
|---|
| LEADER | 01000naa a22002652 4500 | ||
|---|---|---|---|
| 001 | NLM300081103 | ||
| 003 | DE-627 | ||
| 005 | 20231225101738.0 | ||
| 007 | cr uuu---uuuuu | ||
| 008 | 231225s2020 xx |||||o 00| ||eng c | ||
| 024 | 7 | |a 10.1002/ddr.21585 |2 doi | |
| 028 | 5 | 2 | |a pubmed24n1000.xml |
| 035 | |a (DE-627)NLM300081103 | ||
| 035 | |a (NLM)31397505 | ||
| 040 | |a DE-627 |b ger |c DE-627 |e rakwb | ||
| 041 | |a eng | ||
| 100 | 1 | |a Li, He-Min |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Design, synthesis, and biological activity evaluation of BACE1 inhibitors with antioxidant activity |
| 264 | 1 | |c 2020 | |
| 336 | |a Text |b txt |2 rdacontent | ||
| 337 | |a ƒaComputermedien |b c |2 rdamedia | ||
| 338 | |a ƒa Online-Ressource |b cr |2 rdacarrier | ||
| 500 | |a Date Completed 09.07.2021 | ||
| 500 | |a Date Revised 09.07.2021 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a © 2019 Wiley Periodicals, Inc. | ||
| 520 | |a The proteolytic enzyme β-secretase (BACE1) plays a central role in the synthesis of the pathogenic β-amyloid peptides (Aβ) in Alzheimer's disease (AD), antioxidants could attenuate the AD syndrome and prevent the disease progression. In this study, BACE1 inhibitors (D1-D18) with free radical-scavenging activities were synthesized by molecular hybridization of 2-aminopyridine with natural antioxidants. The biological activity evaluation showed that D1 had obvious inhibitory activity against BACE1, and strong antioxidant activity in 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azinobis-(3-ethylbenzthiazoline-6-sulphonate) (ABTS+• ) assay, which could be used as a lead compound for further study | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
| 650 | 4 | |a Alzheimer's disease | |
| 650 | 4 | |a BACE1 | |
| 650 | 4 | |a antioxidant activity | |
| 650 | 4 | |a molecular docking | |
| 650 | 4 | |a molecular hybridization | |
| 650 | 7 | |a Aminopyridines |2 NLM | |
| 650 | 7 | |a Enzyme Inhibitors |2 NLM | |
| 650 | 7 | |a Oxidants |2 NLM | |
| 650 | 7 | |a Amyloid Precursor Protein Secretases |2 NLM | |
| 650 | 7 | |a EC 3.4.- |2 NLM | |
| 650 | 7 | |a Aspartic Acid Endopeptidases |2 NLM | |
| 650 | 7 | |a EC 3.4.23.- |2 NLM | |
| 650 | 7 | |a BACE1 protein, human |2 NLM | |
| 650 | 7 | |a EC 3.4.23.46 |2 NLM | |
| 650 | 7 | |a alpha-aminopyridine |2 NLM | |
| 650 | 7 | |a WSX981HEWU |2 NLM | |
| 700 | 1 | |a Yu, Shao-Peng |e verfasserin |4 aut | |
| 700 | 1 | |a Fan, Tian-Yuan |e verfasserin |4 aut | |
| 700 | 1 | |a Zhong, Yue |e verfasserin |4 aut | |
| 700 | 1 | |a Gu, Ting |e verfasserin |4 aut | |
| 700 | 1 | |a Wu, Wen-Yu |e verfasserin |4 aut | |
| 700 | 1 | |a Zhao, Chao |e verfasserin |4 aut | |
| 700 | 1 | |a Chen, Zhi |e verfasserin |4 aut | |
| 700 | 1 | |a Chen, Min |e verfasserin |4 aut | |
| 700 | 1 | |a Li, Nian-Guang |e verfasserin |4 aut | |
| 700 | 1 | |a Wang, Xiao-Long |e verfasserin |4 aut | |
| 773 | 0 | 8 | |i Enthalten in |t Drug development research |d 1993 |g 81(2020), 2 vom: 15. Apr., Seite 206-214 |w (DE-627)NLM081794991 |x 1098-2299 |7 nnns |
| 773 | 1 | 8 | |g volume:81 |g year:2020 |g number:2 |g day:15 |g month:04 |g pages:206-214 |
| 856 | 4 | 0 | |u http://dx.doi.org/10.1002/ddr.21585 |3 Volltext |
| 912 | |a GBV_USEFLAG_A | ||
| 912 | |a GBV_NLM | ||
| 951 | |a AR | ||
| 952 | |d 81 |j 2020 |e 2 |b 15 |c 04 |h 206-214 | ||