Journal
FUTURE MEDICINAL CHEMISTRY
Volume 15, Issue 1, Pages 189-210Publisher
Newlands Press Ltd
DOI: 10.4155/fmc-2022-0169
Keywords
Alzheimer's disease; cholinesterase; fragment-based drug design; monoamine oxidase B
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This study aimed to develop novel small molecules as selective monoamine oxidase B (MAO-B) inhibitors with cholinesterase inhibition. Compound 6m showed the best neuroprotection, with reversible selective MAO-B inhibition activity (IC50 = 11.54 +/- 0.64 nM). Compounds 6b, 6h, 6j, 6n and 6p also appeared as potent and selective MAO-B inhibitors with anti-AChE activity.
Aim: Multitargeted drugs are essential for the treatment of various neurodegenerative disorders, because of their complex nature. This study aimed to develop novel small molecules as selective monoamine oxidase B (MAO-B) inhibitors with cholinesterase inhibition. Materials & methods: With the help of fragment-based drug design, some 4-oxo-N-4-diphenyl butanamides were designed and synthesized as MAO-B inhibitors with anti-acetylcholinesterase (AChE) activity. Results: Compound 6m showed the best neuroprotection, with reversible selective MAO-B inhibition activity (IC50 = 11.54 +/- 0.64 nM). Compounds 6b, 6h, 6j, 6n and 6p (IC50 = 20.90 +/- 0.50, 17.25 +/- 0.90, 15.85 +/- 0.16, 16.81 +/- 0.85 and 25.19 +/- 0.17 nM, respectively) also appeared as potent and selective MAO-B inhibitors with anti-AChE activity. Conclusion: The present study suggests potent, neuroprotective and nontoxic lead compounds as selective MAO-B inhibitors with anti-AChE activity.
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