Introduction

The present invention is related to boronated compounds with neuroprotective, antiplatelet, antitumor, and antimicrobial activities for the treatment of diseases and conditions associated to oxidative stress.

Technical features

The inventors have designed and synthesized novel boron-based hybrids (BBH) which have proved to be effective as neuroprotective agents for the treatment of neurodegenerative diseases mainly related to oxidative stress. The neuroprotective profile of the novel BBH (BLA) was evaluated in vitro using Aβ1-42-treated-SH-SY5Y cells. Results showed that BLA (a novel boron-based hybrid containing an antioxidant portion) inhibited cell death induced by Aβ1-42-exposure in differentiated SH-SY5Y cells, resulting in an increase in the cell viability by 33-71 % (MTT and LDH assays) at the range concentrations of 25-100 μM (Figure). Antioxidant assays demonstrated a good a capability of BLA to counteract the oxidative status. Moreover, BLA possessed a significant ability to inhibit acetyl cholinesterase (AChE) (22.96% at 50 µM), an enzyme whose enzymatic activity is increased in Alzheimer-affected patients. These data confirmed that BLA is a multi-target boronated ligand affecting simultaneously multiple target sites involved in Alzheimer’s disease.

Possible Applications

• BBH are new structural scaffolds for the development of novel drugs for the management of Alzheimer’s Disease;
• Neurodegenerative diseases, notably diseases related to oxidative stress such as Alzheimer’s disease.

Advantages

• No toxicity and limitation in the dosage compared to other boronated derivatives;
• Better physical-chemical properties (solubility and lipophilia);
• Ability to cross biological barriers;
• Interfere with the deposition of protein aggregates that are formed during neurodegenerative processes.