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Pune, India – In a significant breakthrough, scientists at the Agharkar Research Institute (ARI), an autonomous institution under the Department of Science and Technology, have synthesized new molecules showing promise for treating Alzheimer’s disease (AD). These molecules, developed through a combination of synthetic chemistry, computational techniques, and in-vitro testing, could pave the way for more effective therapies for neurodegenerative disorders like Alzheimer’s.
The research team at ARI leveraged an innovative one-pot, three-component reaction with high synthetic yields to create these novel molecules. Using in-vitro screening, they evaluated the potency and toxicity levels, ensuring the molecules’ safety and potential effectiveness. Notably, these new molecules showed promising efficacy as cholinesterase inhibitors—a class of drugs known to enhance memory and learning by increasing levels of acetylcholine, a vital chemical messenger.
“The molecules were found to be non-toxic and effective against cholinesterase enzymes,” explained the ARI team. “The lead compound demonstrated a strong selectivity ratio for acetylcholinesterase over butyrylcholinesterase, enhancing its therapeutic potential for Alzheimer’s patients.”
These molecules also displayed good stability, binding well within the enzyme’s active site due to favorable interactions with amino acids, as revealed through molecular dynamics simulations. Researchers believe this stability could contribute to the molecules’ effectiveness in the brain, where Alzheimer’s impacts cholinergic pathways critical to memory and cognition.
The team further noted that these molecules are dual cholinesterase inhibitors, targeting both acetylcholinesterase and butyrylcholinesterase, enhancing their therapeutic applicability in treating Alzheimer’s and potentially other neurodegenerative diseases such as Parkinson’s.
“These molecules could serve as the foundation for developing dual anti-cholinesterase drugs, potentially in combination with other therapies,” said the researchers. Future work will explore synthesizing additional compounds, including substituted carbazole and chromene analogues, which may have even greater anti-Alzheimer’s properties.
Alzheimer’s, a disease driven by a complex interplay of genetic, environmental, and biochemical factors, affects nearly 60-70% of the approximately 55 million people globally who suffer from dementia. In India alone, the prevalence of Alzheimer’s has increased significantly, with family caregivers and healthcare professionals alike awaiting better therapeutic options.
This promising research brings hope for new AD treatments that are urgently needed as the global population ages. Continued exploration and optimization of these molecules at ARI mark an important step toward expanding India’s contributions to neurodegenerative disease research and could place the country at the forefront of innovative Alzheimer’s treatments.
