Discovery of palmatine derivatives as potent neuroprotective agents

Abstract

Alzheimer’s disease is a neurodegenerative disorder characterized by the presence of neurodegenerative lesions and cognitive impairment. In this study, a series of novel palmatine derivatives were designed and synthesized through the introduction of a heteroatom using carbodiimide-mediated condensation. The synthesized compounds were then screened for toxicity and potency, leading to the identification of compound 2q, which exhibited low toxicity and high potency. Our findings demonstrated that compound 2q displayed significant neuroprotective activity in vitro, emerging as a promising candidate for Alzheimer’s disease treatment.

Keywords:

• Alzheimer’s disease
• palmatine
• synthesis
• neuroprotective

Disclosure statement

No potential conflict of interest was reported by the author(s).

Additional information

Funding

This study was financially supported by the Beijing Municipal Research Ward Construction Project (BCRW202101), National Natural Science Foundation of China [grant no.8174106, 31970508 and 31900380] CAMS Innovation Fund for Medical Sciences [CIFMS, 2021-I2M-1-034], and the Drug Innovation Major Project [2018ZX09711-001-005].