Potent, easily synthesized huperzine A-tacrine hybrid acetylcholinesterase inhibitors

Paul R. Carlier; Da Ming Du; Yifan Han; Jing Liu; Yuan Ping Pang

doi:10.1016/S0960-894X(99)00396-0

Potent, easily synthesized huperzine A-tacrine hybrid acetylcholinesterase inhibitors

Paul R. Carlier^*, Da Ming Du, Yifan Han, Jing Liu, Yuan Ping Pang

^*Corresponding author for this work

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

89 Citations (Scopus)

Abstract

Hybrid acetylcholinesterase inhibitors composed of a key fragment of huperzine A and an intact tacrine unit were prepared. The syntheses are quite direct, proceeding in a maximum of 4 linear steps from commercially available starting materials. The optimum hybrid inhibitor (±)-9g is 13-fold more potent than (-)-huperzine A, and 25-fold more potent than tacrine.

Original language	English
Pages (from-to)	2335-2338
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	9
Issue number	16
DOIs	https://doi.org/10.1016/S0960-894X(99)00396-0
Publication status	Published - 16 Aug 1999
Externally published	Yes

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10.1016/S0960-894X(99)00396-0

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abstract = "Hybrid acetylcholinesterase inhibitors composed of a key fragment of huperzine A and an intact tacrine unit were prepared. The syntheses are quite direct, proceeding in a maximum of 4 linear steps from commercially available starting materials. The optimum hybrid inhibitor (±)-9g is 13-fold more potent than (-)-huperzine A, and 25-fold more potent than tacrine.",

author = "Carlier, {Paul R.} and Du, {Da Ming} and Yifan Han and Jing Liu and Pang, {Yuan Ping}",

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AU - Carlier, Paul R.

AU - Du, Da Ming

AU - Han, Yifan

AU - Liu, Jing

AU - Pang, Yuan Ping

PY - 1999/8/16

Y1 - 1999/8/16

N2 - Hybrid acetylcholinesterase inhibitors composed of a key fragment of huperzine A and an intact tacrine unit were prepared. The syntheses are quite direct, proceeding in a maximum of 4 linear steps from commercially available starting materials. The optimum hybrid inhibitor (±)-9g is 13-fold more potent than (-)-huperzine A, and 25-fold more potent than tacrine.

AB - Hybrid acetylcholinesterase inhibitors composed of a key fragment of huperzine A and an intact tacrine unit were prepared. The syntheses are quite direct, proceeding in a maximum of 4 linear steps from commercially available starting materials. The optimum hybrid inhibitor (±)-9g is 13-fold more potent than (-)-huperzine A, and 25-fold more potent than tacrine.

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U2 - 10.1016/S0960-894X(99)00396-0

DO - 10.1016/S0960-894X(99)00396-0

M3 - Article

C2 - 10476864

AN - SCOPUS:0033575679

SN - 0960-894X

VL - 9

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EP - 2338

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 16

ER -

Potent, easily synthesized huperzine A-tacrine hybrid acetylcholinesterase inhibitors

Abstract

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