Tổng hợp các hợp chất bis-heterocyclic chứa thieno[2,3-b]thiophene - Các dẫn xuất dược lý mới
Tóm tắt
Các dẫn xuất thiênethiofen đại diện cho một lớp hợp chất quan trọng với nhiều hoạt tính sinh học khác nhau. Chúng tôi mô tả ở đây quy trình tổng hợp một loạt hợp chất mới chứa thieno[2,3-b]thiophene 3–7. Tất cả các hợp chất đã được đánh giá về tiềm năng chống oxy hóa in vitro, khả năng ức chế α-glucosidase và β-glucuronidase cũng như hoạt tính chống ung thư đối với dòng tế bào PC-3. Các hợp chất 2b (IC50 = 1.3 ± 0.2 μM), 5a (IC50 = 2.3 ± 0.4 μM) và 5b (IC50 = 8.7 ± 0.1 μM) cho thấy khả năng ức chế mạnh mẽ enzyme β-glucuronidase, hoạt động hiệu quả hơn so với tiêu chuẩn d-saccharic acid 1,4-lactone (IC50 = 45.8 ± 2.5 μM). Các hợp chất 5a (IC50 = 22.0 ± 0.3 μM) và 5b (IC50 = 58.4 ± 1.2 μM) cũng cho thấy khả năng ức chế α-glucosidase mạnh mẽ so với thuốc tiêu chuẩn (acarbose, IC50 = 841 ± 1.7 μM).
Từ khóa
Tài liệu tham khảo
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