Tổng hợp và thử hoạt tính kháng khuẩn của các dẫn chất 1,3-benzodioxole

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Tác giả: Ngọc Phương Kiều Nguyễn, Ngọc Châu Trần, Thanh Thảo Vũ

Ngôn ngữ: Vie

Ký hiệu phân loại:

Thông tin xuất bản: Khoa học & công nghệ Việt Nam 2023

Mô tả vật lý: 22 - 27

Bộ sưu tập: Metadata

ID: 408473

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Tóm tắt
Chủ đề

Trước tình trạng đề kháng kháng sinh ngày càng gia tăng hiện nay, việc nghiên cứu các khung cấu trúc mới có tác dụng ức chế sự phát triển của vi khuẩn là rất cần thiết. Cấu trúc 1,3-benzodioxole với nhiều hoạt tính sinh học tiềm năng là đối tượng chính của nghiên cứu này. Từ nguyên liệu piperonal, 5 dẫn chất mang khung cấu trúc 1,3-benzodioxole được tổng hợp bằng các phản ứng hóa học đa dạng khác nhau. Cấu trúc của sản phẩm được xác định bằng các phương pháp quang phổ. Hoạt tính kháng khuẩn in vitro được khảo sát bằng phương pháp khuếch tán trong thạch trên 5 chủng vi khuẩn: Escherichia coli, Pseudomonas aeruginosa, Enterococcus faecalis, Staphylococcus aureus nhạy cảm methicillin (MSSA) và tụ cầu vàng đề kháng methicillin (MRSA). Dẫn chất base Schiff (2) thể hiện khả năng ức chế 4/5 chủng vi khuẩn thử nghiệm, trong đó có MRSA. Nghiên cứu dự đoán đích tác động và mô phỏng gắn kết in silico gợi ý khả năng gắn kết của chất (2) trên enzyme FabH của vi khuẩn. Kết quả nghiên cứu gợi ý về sự phối hợp giữa nhóm base Schiff và khung 1,3-benzodioxole trong phát triển các chất kháng khuẩn mới., Tóm tắt tiếng anh, Novel chemical entities are urgently needed to develop new antibacterial agents in order to tackle the increasing antibiotic resistance. This study focuses on the 1,3-benzodioxole scaffold with promising biological activities in the literature. Five 1,3-benzodioxole containing derivatives were synthesised from piperonal as starting material by various chemical reactions. Their structures were elucidated by standard spectroscopic methods. The in vitro antibacterial activities were studied by agar diffusion method against 5 pathogenic strains: Escherichia coli, Pseudomonas aeruginosa, Enterococcus faecalis, methicillin-susceptible Staphylococcus aureus (MSSA), and methicillin-resistant Staphylococcus aureus (MRSA). The Schiff base derivative (2) showed the ability to inhibit 4/5 tested strains, including MRSA. The target prediction study suggested the in silico binding ability of (2) on the bacterial FabH enzyme. These results demonstrated that novel 1,3-benzodioxole derivatives containing Schiff bases could be further studied as new antibacterial structures.

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