Docking-based design and synthesis of galantamine–camphane hybrids as inhibitors of acetylcholinesterase,Chemical Biology & Drug Design

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Docking-based design and synthesis of galantamine–camphane hybrids as inhibitors of acetylcholinesterase
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2017-05-12 07:16:10 , DOI: 10.1111/cbdd.12991
Georgi Stavrakov ₁ , Irena Philipova ₂ , Dimitrina Zheleva-Dimitrova ₁ , Iva Valkova ₁ , Evdokiya Salamanova ₃ , Spiro Konstantinov ₁ , Irini Doytchinova ₁

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The galantamine fragment of the galantamine–camphane hybrids bind the catalytic site of acetylcholinesterase, while the camphane fragment fits in the peripheral anionic site, where the Ω-loop of amyloid beta peptide binds to the enzyme. The inhibitor “closes” the binding site by causing a shift of Trp286 and prevents the amyloid beta peptide from binding.

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