The Synthesis of Certain Derivatives and Analogues of (−)- and (+)-Galanthamine and an Assessment of their Capacities to Inhibit Acetylcholine Esterase | Zendy

Joshua N. Buckler | Zendy; Ehab S. Taher | Zendy; Nicholas J Fraser | Zendy; Anthony C. Willis | Zendy; Paul D. Carr | Zendy; Colin J. Jackson | Zendy; Martin G. Banwell | Zendy

Open Access

The Synthesis of Certain Derivatives and Analogues of (−)- and (+)-Galanthamine and an Assessment of their Capacities to Inhibit Acetylcholine Esterase

Author(s) -

Joshua N. Buckler,

Ehab S. Taher,

Nicholas J Fraser,

Anthony C. Willis,

Paul D. Carr,

Colin J. Jackson,

Martin G. Banwell

Publication year - 2017

Publication title -

the journal of organic chemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.2

H-Index - 228

eISSN - 1520-6904

pISSN - 0022-3263

DOI - 10.1021/acs.joc.7b01062

Subject(s) - chemistry , acetylcholine , esterase , acetylcholinesterase , cholinesterase , pharmacology , stereochemistry , biochemistry , enzyme , medicine

Syntheses of certain di- and mono-oxygenated derivatives (e.g., 2 and 3, respectively) and analogues (e.g., 4, a D-ring monoseco-analogue of 2) of both the (-)- and (+)-enantiomeric forms of the alkaloid galanthamine [(-)-1] are reported. All have been assessed for their capacities to inhibit acetylcholine esterase but, in contrast to the predictions from docking studies, none bind strongly to this enzyme.

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