Synthesis, Molecular Structure, and Biological Properties of Novel 9 <i>H</i> ‐Carbazole‐Derived 1,3‐Thiazoles
ABSTRACT A series of novel 1,3‐thiazole derivatives (5a–5j) was synthesized and fully characterized by FT‐IR, NMR, and HR‐MS. The compounds were evaluated for antifungal activity and α‐glucosidase inhibition. Compounds 5e and 5j showed notable antifungal effects against Trichophyton rubrum and T. mentagrophytes . Among the series, compound 5g exhibited the most potent α‐glucosidase inhibitory activity (IC 50 = 8.25 ± 0.12 μM), significantly stronger than acarbose. Molecular docking and molecular dynamics simulations supported its stable binding within the enzyme active site, while DFT calculations suggested favorable electronic features associated with enhanced activity. In vivo evaluation further confirmed its glucose‐lowering effect in a zebrafish model. Overall, these findings identify compound 5g as a promising lead and highlight the 1,3‐thiazole scaffold as a valuable platform for the development of new α‐glucosidase inhibitors.
Authors
- Nguyễn Thị Mai Thơ
- Nguyen Ngoc Huyen Tran
- Nguyen Duy Khanh
- Nguyen Van Son
- Nguyen Thi Nhat Thang
- Tran Nguyen Minh An
- Nguyen Thi Hong Anh
- Nguyen Van Thoi
- Tran Thi Thanh Truc
Institutions
- Industrial University of Ho Chi Minh City (VN)
- Ho Chi Minh City University of Industry and Trade (VN)
Publication Details
- Journal
- Journal of Heterocyclic Chemistry
- Published
- 2026-05-27
- DOI
- https://doi.org/10.1002/jhet.70216
- Primary Topic
- Natural Antidiabetic Agents Studies
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- National Foundation for Science and Technology Development