TY - JOUR
T1 - Discovery of alkenylboronic acids as neuroprotective agents affecting multiple biological targets involved in Alzheimer's disease
AU - Jiménez-Aligaga, Karim
AU - Bermejo-Bescós, Paloma
AU - Martín-Aragón, Sagrario
AU - Csákÿ, Aurelio G.
N1 - Funding Information:
This work was supported by grant CTQ2010-6170 from the Ministerio de Economía y Competitividad from the government of Spain. We thank Fundación Folch for a pre-doctoral grant to K. J.-A.
PY - 2013/1/15
Y1 - 2013/1/15
N2 - Alkenylboronic acids have shown important biological activities that contribute to neuroprotection. We have determined their influence on the β-amyloid (βA) aggregation process, β-secretase and acethylcholinesterase activities on cell-free systems, on the redox and lipid peroxidation status, and on the vulnerability to apoptotic death in an APPswe neuroblastoma cell line, before and after hydrogen peroxide treatment. We have discovered that 2-arylvinylboronic acids and some of their esters possess a set of properties which makes them highly useful as neuroprotective agents affecting multiple biological targets involved in AD. These properties are not paralleled by the related 2-arylboronic acids.
AB - Alkenylboronic acids have shown important biological activities that contribute to neuroprotection. We have determined their influence on the β-amyloid (βA) aggregation process, β-secretase and acethylcholinesterase activities on cell-free systems, on the redox and lipid peroxidation status, and on the vulnerability to apoptotic death in an APPswe neuroblastoma cell line, before and after hydrogen peroxide treatment. We have discovered that 2-arylvinylboronic acids and some of their esters possess a set of properties which makes them highly useful as neuroprotective agents affecting multiple biological targets involved in AD. These properties are not paralleled by the related 2-arylboronic acids.
KW - Boronic acids
KW - Caspase
KW - Glutathione
KW - Lipid peroxidation
KW - β-Amyloid fibrillogenesis
UR - http://www.scopus.com/inward/record.url?scp=84871712446&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2012.11.068
DO - 10.1016/j.bmcl.2012.11.068
M3 - Artículo
C2 - 23219701
AN - SCOPUS:84871712446
SN - 0960-894X
VL - 23
SP - 426
EP - 429
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 2
ER -