Highly Efficient Synthesis of 1,3-Dihydroxy-2-carboxycarbazole and Its Neuroprotective Effects.

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.

• Authors: Kai Liu, Shijun Zhang
• Journal: ACS medicinal chemistry letters (ACS Med Chem Lett) Vol. 6 Issue 8 Pg. 894-7 (Aug 13 2015) ISSN: 1948-5875 [Print] United States
• PMID: 26288690 (Publication Type: Journal Article)