Highly Efficient Synthesis of 1,3-Dihydroxy-2-carboxycarbazole and Its Neuroprotective Effects
1Department of Medicinal Chemistry, Virginia Commonwealth University , Richmond, Virginia 23298, United States.
Abstract:
Carbazoles represent a family of tricyclic compounds that widely appeared in nature. Numerous studies have revealed a diverse array of bioactivity associated with this scaffold. In the present study, a novel and highly efficient methodology for preparing 1,3-dihydroxy-2-carboxycarbazole from indole-3-acetic acid and Meldrum's acid was developed. Furthermore, biological characterization demonstrated that this multisubstituted carbazole analogue exhibited inhibitory activity on Aβ aggregation, antioxidative properties, and promising neuroprotective activities in a cellular model of Alzheimer's disease, thus further supporting the valuable application of this synthetic methodology in search for effective neuroprotectants.
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