Oximes [electronic resource] : Inhibitors of Human Recombinant Acetylcholinesterase. A Structure-Activity Relationship (SAR) Study

• Ngôn ngữ: eng
• Ký hiệu phân loại: 574.87 [Unassigned]
• Thông tin xuất bản: Washington, D.C. : Oak Ridge, Tenn. : United States. Dept. of Energy. Office of Science ; Distributed by the Office of Scientific and Technical Information, U.S. Dept. of Energy, 2013
• Mô tả vật lý: Size: p. 16882-16900 : , digital, PDF file.
• Bộ sưu tập: Metadata
• ID: 261496
• Chủ đề: 1. 59 basic biological sciences; 2. 60 applied life sciences; 3. Acetylcholinesterase; 4. Biochemistry & molecular biology; 5. Chemistry; 6. Inhibitors; 7. Oximes; 8. Sar study

Tóm tắt

Acetylcholinesterase (AChE) reactivators were developed for the treatment of organophosphate intoxication. Standard care involves the use of anticonvulsants (e.g., diazepam), parasympatolytics (e.g., atropine) and oximes that restore AChE activity. However, oximes also bind to the active site of AChE, simultaneously acting as reversible inhibitors. The goal of the present study is to determine how oxime structure influences the inhibition of human recombinant AChE (hrAChE). Therefore, 24 structurally different oximes were tested and the results compared to the previous eel AChE (EeAChE) experiments. Structural factors that were tested included the number of pyridinium rings, the length and structural features of the linker, and the number and position of the oxime group on the pyridinium ring.