Highly Efficient Synthesis of 1,3-Dihydroxy-2-carboxycarbazole and Its Neuroprotective Effects.
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.
Department of Medicinal Chemistry, Virginia Commonwealth University , Richmond, Virginia 23298, United States.
Kai
K
Liu
Department of Medicinal Chemistry, Virginia Commonwealth University , Richmond, Virginia 23298, United States.
Shijun
S
Zhang
Aβ oligomers; Carbazole derivative; Meldrum’s acid; antioxidant; neuroprotection; synthesis