Synthesis of (±)-10,10-dimethylhuperzine A - A huperzine analogue possessing a slower enzyme off-rate

Alan P. Kozikowski; Qingjie Ding; Ashima Saxena; Bhupendra P. Doctor

doi:10.1016/0960-894X(96)00012-1

Synthesis of (±)-10,10-dimethylhuperzine A - A huperzine analogue possessing a slower enzyme off-rate

Alan P. Kozikowski, Qingjie Ding, Ashima Saxena, Bhupendra P. Doctor

Research output: Contribution to journal › Article › peer-review

32 Scopus citations

Abstract

The synthesis of (±)-10,10-dimethylhuperzine A is reported together with its kinetic (k_on and k_off) and dissociation constants for the inhibition of fetal bovine serum acetylcholinesterase. While somewhat more potent than (±)-huperzine A, the dimethyl analogue shows a slower off-rate from AChE, a result that may be of potential therapeutic value.

Original language	English (US)
Pages (from-to)	259-262
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	6
Issue number	3
DOIs	https://doi.org/10.1016/0960-894X(96)00012-1
State	Published - 1996
Externally published	Yes

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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title = "Synthesis of (±)-10,10-dimethylhuperzine A - A huperzine analogue possessing a slower enzyme off-rate",

abstract = "The synthesis of (±)-10,10-dimethylhuperzine A is reported together with its kinetic (kon and koff) and dissociation constants for the inhibition of fetal bovine serum acetylcholinesterase. While somewhat more potent than (±)-huperzine A, the dimethyl analogue shows a slower off-rate from AChE, a result that may be of potential therapeutic value.",

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AU - Kozikowski, Alan P.

AU - Ding, Qingjie

AU - Saxena, Ashima

AU - Doctor, Bhupendra P.

PY - 1996

Y1 - 1996

N2 - The synthesis of (±)-10,10-dimethylhuperzine A is reported together with its kinetic (kon and koff) and dissociation constants for the inhibition of fetal bovine serum acetylcholinesterase. While somewhat more potent than (±)-huperzine A, the dimethyl analogue shows a slower off-rate from AChE, a result that may be of potential therapeutic value.

AB - The synthesis of (±)-10,10-dimethylhuperzine A is reported together with its kinetic (kon and koff) and dissociation constants for the inhibition of fetal bovine serum acetylcholinesterase. While somewhat more potent than (±)-huperzine A, the dimethyl analogue shows a slower off-rate from AChE, a result that may be of potential therapeutic value.

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ER -

Synthesis of (±)-10,10-dimethylhuperzine A - A huperzine analogue possessing a slower enzyme off-rate

Abstract

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