Tổng hợp, phân tích và đánh giá dược lý của các dẫn xuất thiourea

Walter de Gruyter GmbH - Tập 18 Số 1 - Trang 764-777 - 2020
Sumaira Naz1, Muhammad Zahoor1, Muhammad Umar1, Saad Alghamdi2, Muhammad Umar Khayam Sahibzada3, Wasim UlBari1
1Department of Chemistry, University of Malakand, Chakdara, Dir Lower, 18800 KPK, Pakistan
2Department of Laboratory Medicine, Faculty of Applied Medical Sciences, Umm Al-Qura University, P.O. Box 715, Makkah 21955, Saudi Arabia
3Department of Pharmacy, Sarhad University of Science and Information Technology, Peshawar, KPK, 25000, Pakistan

Tóm tắt

Tóm tắt

Các hợp chất thiourea và dẫn xuất của chúng là các hợp chất có chứa lưu huỳnh hữu cơ với nhiều ứng dụng trong các lĩnh vực như tổng hợp hữu cơ và ngành công nghiệp dược phẩm. Các dẫn xuất thiourea đối xứng đã được tổng hợp qua phản ứng của nhiều loại anilin với CS2. Các hợp chất được tổng hợp đã được đặc trưng bằng các kỹ thuật quang phổ UV-visible và cộng hưởng từ hạt nhân (NMR). Các hợp chất này đã được sàng lọc để kiểm tra khả năng ức chế in vitro của các enzym α-amylase, α-glucosidase, acetylcholinesterase (AChE) và butyrylcholinesterase (BuChE), cũng như tiềm năng kháng khuẩn và chống oxy hóa của chúng. Các hợp chất này đã được cho ăn cho chuột trắng Swiss đực để đánh giá tác động độc hại và khả năng ức chế glucose-6-phosphatase (G6Pase). Các nghiên cứu kháng khuẩn cho thấy hợp chất 4 hoạt động hiệu quả hơn đối với các chủng vi khuẩn được chọn. Hợp chất 1 có hoạt tính tốt hơn đối với các gốc tự do 2,2-diphenyl-1-picrylhydrazyl và 2,2’-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), AChE, BuChE và α-glucosidase. Hợp chất 2 có tác dụng mạnh hơn đối với α-amylase và G6Pase. Các nghiên cứu về độ độc cho thấy rằng hợp chất 4 là an toàn vì không gây ra tác dụng độc hại lên bất kỳ các thông số huyết học và sinh hóa nào hoặc trên mô gan của các động vật thực nghiệm ở bất kỳ liều lượng nào đã được nghiên cứu. Các hợp chất được tổng hợp cho thấy tiềm năng kháng khuẩn và chống oxy hóa đầy triển vọng và hoạt động rất mạnh (cả in vitroin vivo) đối với G6Pase, và hoạt động trung bình đối với các enzym khác được chọn trong nghiên cứu này.

Từ khóa


Tài liệu tham khảo

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