Synthesis and Cholinesterase Inhibitory Activites of Analogues of Marine Product Anithiactins C
Three analogues of Marine natural product Anithiactins C were designed and synthesized.The structures of the compounds were confirmed using NMR,X-single crystal diffraction techniques and in-frared spectroscopy.The single crystal diffraction results showeded that the compound 2-(4-(benzyloxy)phenyl)-N,N-dipropylthiazole-4-carboxamide belonged to the trigonal crystal system,P-1 space group,and the compound 2-(4-(benzyloxy)phenyl)-N-cyclohexylthiazole-4-carboxamide belonged to the mono-clinic character,P21/c space group.The cholinesterase inhibitory activity of the compounds was assayed using the Ellman method,among this series,compound 2-(4-(benzyloxy)phenyl)-N-cyclohexylthiazole-4-carboxamide showed the best acetyl cholinesterase inhibitory activity with an IC50 value of(53.99±0.13)μmol/L.The molecular docking results indicated that the compound acted on both the acetyl cho-linesterase PAS and CAS sites,and could be further developed as a dual-site binding acetylcholine inhibi-tor.
analogue of Anithiactins Csynthesischaracterizationcholinesterase inhibitory activites
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