Tổng hợp và đánh giá hoạt tính kháng khuẩn của một số dẫn xuất naphthalene-1,3,4-oxadiazole

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Tác giả: Thị Bửu Huê Bùi, Thị Cẩm Tuyết Ngô, Thanh Trung Nguyễn, Thị Cẩm Hồng Nguyễn, Thị Ngọc Yến Nguyễn, Tuấn Vũ Nguyễn, Việt Cường Trang, Trung Hiếu Võ

Ngôn ngữ: vie

Ký hiệu phân loại: 547.8 Other organic substances

Thông tin xuất bản: Khoa học (Đại học Cần Thơ), 2018

Mô tả vật lý: 35-41

Bộ sưu tập: Metadata

ID: 491963

Thêm vào giỏ

1,3,4-oxadiazole có nhiều hoạt tính sinh học bao gồm kháng khuẩn, kháng nấm, kháng viêm, giảm đau, hạ lipid máu, kháng ung thư, chống co giật, chống đái tháo đường, kháng virus và chống loét. Trong nghiên cứu này, hai dẫn xuất 2-phenyl-5-(3,4,5-trimethoxyphenyl)-1,3,4-oxadiazole và 2-(4-methoxy-6-methylnaphthalen-2-yl)-5-phenyl-1,3,4-oxadiazole đã được tổng hợp thành công với hiệu suất rất cao. Phương pháp tổng hợp được sử dụng là phản ứng ghép vòng dẫn xuất acylhydrazone tạo nhân 1,3,4-oxadiazole sử dụng iodine làm tác nhân oxy hóa dưới sự hiện diện của potassium carbonate. Các điều kiện của phản ứng này cũng áo dụng tốt với chất nền là acylhydrazone thô thu được từ sự ngưng tụ giữa aldehyde và hydrazide. Đánh giá hoạt tính kháng khuẩn của hai dẫn xuất cho thấy hai hợp chất này có khả năng kháng lại ba chủng vi khuẩn: Escherichia coli, Staphylococcus aureus và Bacillus cereus.1,3,4-Oxadizole exhibites a wide range of biological activities including antibacterial, antifungal, antiinflammatory, analgesic, hypolipidemic, anticancer, anticonvulsant, anti-diabetic, antiviral and ulcerogenic activities. In this study, two derivatives of 2-phenyl-5-(3,4,5-trimethoxyphenyl)-1,3,4-oxadiazole (6a) and 2-(4-methoxy-6-methylnaphthalen-2-yl)-5-phenyl-1,3,4-oxadiazole (8b) have been successfully synthesized in very good yields. The synthesis key step was cyclization of acylhydrazones into 1,3,4-oxadiazoles using stoichiometric amount of molecular iodine in potassium carbonate. The synthetic method also worked well with crude acylhydrazone substrates obtained from the condensation of aldehydes and hydrazides. Antimicrobial activity evaluation of two derivatives (6a) and (8b) showed that these two compounds possessed activity against three bacterial strains of Escherichia coli, Staphylococcus aureus and Bacillus cereus.

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