1. Alkynyl and β-ketophosphonates: Selective and potent butyrylcholinesterase inhibitors.
- Author
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Cavallaro, Valeria, Moglie, Yanina F., Murray, Ana P., and Radivoy, Gabriel E.
- Subjects
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CHOLINESTERASES , *ORGANOPHOSPHORUS compounds , *PHOSPHONATES , *ACETYLENE , *ENZYMATIC analysis - Abstract
A series of thirty-three alkynyl and β-ketophosphonates were evaluated for their in vitro acetyl- and butyryl-cholinesterase (AChE and BChE) inhibitory activities using Ellman’s spectrophotometric method. None of the examined compounds inhibited AChE activity at tested concentrations while twenty-nine of them showed significant and selective inhibition of BChE with IC 50 values between 38.60 µM and 0.04 µM. In addition, structure-activity relationships were discussed. The most effective inhibitors were the dibutyl o -methoxyphenyl alkynylphosphonate 3dc and dibutyl o -methoxyphenyl β-ketophosphonate 4dc . Activities of most potent compounds were also compared with a commercial organophosphorus compound. These results could inspire the design of new inhibitors with stronger activity against BChE. [ABSTRACT FROM AUTHOR]
- Published
- 2018
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