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Correia, I; Bezzenine, N; Ronzani, N; Platzer, N; Beloeil, JC; Doan, BT

Study of inclusion complexes of acridine with ß- and (2,6-di-O-methyl)-ß-cyclodextrin by use of solubility diagrams and NMR spectroscopy

Journal of Physical Organic Chemistry 15 (9) 647-659

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Previous molecular modeling studies, in our laboratory, have shown that some esters of type RCOO(CH2)(n)C5H5N+Cl- are potentially active against Alzheimer’s disease. We have also demonstrated that acridine, which has strong anticholinesterase activity appears to be a suitable R substituent. The main obstacle to the possible pharmaceutical application of these compounds is their limited solubility in water, which is due to the poor aqueous solubility of acridine itself (0.26 mM). Inclusion complexation with cyclodextrins may overcome this problem.