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Updated: Jun 27, 2026

Preparation of Enantiopure Non-Activated Aziridines and Synthesis of Biemamide B, D, and epiallo-Isomuscarine
Published on: June 13, 2022
Carbazole-Based Ester Derivatives as Potential α-Glucosidase Inhibitors; Synthesis, Biological Evaluation, and
Leyla Kaya1, Mehmet F Saglam2, Rabia Sarıbas2
1Department of Pharmaceutical Toxicology, Faculty of Pharmacy, Zonguldak Bulent Ecevit University, Zonguldak 67600, Türkiye.
Abstract:
In this study, a new range of carbazole linked mono- and bis-ester derivatives were successfully synthesized and evaluated for their in vitro anti-diabetic activity through α-amylase and α-glucosidase inhibition. The synthetic approach for the preparation of mono-esters 5a-j and bis-esters 7a-j was achieved by the reaction of carbazole-3-methanol 4 and carbazole-3,6-dimethanol 6 with a variety of acyl chlorides. The targeted compounds displayed generally weak α-amylase inhibition but significant and selective inhibition against α-glucosidase. Among them, 7a, 7g, and 7j exhibited dual inhibitory activity, while 7f was selective for α-glucosidase, and 7d and 5g for α-amylase. Notably, 7g was the most potent compound (IC50 = 22.79 µM), surpassing Acarbose. In addition, molecular docking studies of the synthesized compounds were carried out to investigate their interactions with the α-glucosidase enzyme. Overall, targeted carbazole-based ester derivatives show promising results as selective anti-diabetic agents.
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