Show simple item record

dc.contributor.authorCarradori, Simone
dc.contributor.authorPetzer, Anél
dc.contributor.authorPetzer, Jacobus P.
dc.contributor.authorOrtuso, Francesco
dc.contributor.authorBagetta, Donatella
dc.identifier.citationCarradori, S. et al. 2018. Design, synthesis and biochemical evaluation of novel multi-target inhibitors as potential anti-Parkinson agents. European journal of medicinal chemistry, 143:1543-1552. []en_US
dc.identifier.issn1768-3254 (Online)
dc.description.abstractNew 4-(3-nitrophenyl)thiazol-2-ylhydrazone derivatives are proposed as dual-target-directed monoamine oxidase B (MAO-B) and acetylcholinesterase (AChE) inhibitors, as well as antioxidant agents, for the treatment of neurodegenerative disorders such as Parkinson's disease. Rational molecular design, target recognition and predicted pharmacokinetic properties have been evaluated by means of molecular modelling. Based on these properties, compounds were synthesized and evaluated in vitro as MAO-B and AChE inhibitors, and compared to the activities at their corresponding isozymes, monoamine oxidase A (MAO-A) and butyrylcholinesterase (BuChE), respectively. Anti-oxidant properties, potentially useful in the treatment of neurodegenerative disorders, have been also investigated in vitro. Among the evaluated compounds, three inhibitors may be considered as promising dual inhibitors of MAO-B and AChE, in vitro. MAO-B inhibition was also shown to be competitive and reversible for compound 19en_US
dc.subjectRational designen_US
dc.subjectParkinson's diseaseen_US
dc.subjectSelective monoamine oxidase inhibitorsen_US
dc.subjectSelective cholinesterase inhibitorsen_US
dc.subjectAntioxidant agentsen_US
dc.titleDesign, synthesis and biochemical evaluation of novel multi-target inhibitors as potential anti-Parkinson agentsen_US
dc.contributor.researchID12264954 - Petzer, Anél
dc.contributor.researchID10727388 - Petzer, Jacobus Petrus

Files in this item


There are no files associated with this item.

This item appears in the following Collection(s)

Show simple item record