Synthesis of tacrine analogues and their structure-activity relationships

Proctor, G R and Harvey, A L (2000) Synthesis of tacrine analogues and their structure-activity relationships. Current Medicinal Chemistry, 7 (3). pp. 295-302. ISSN 0929-8673

Abstract

Three man synthetic routes to analogues of tacrine are described: reaction of anthranilonitriles with cyclohexanone and other ketones, reaction of various anilines with alpha-cyanoketones, and reactions involving anilines and cyclic beta-ketoesters. Although tacrine has a wide range of pharmacological effects, it is best known as an inhibitor of cholinesterase enzymes. Many of the analogues that have been made have not been tested against acetylcholinesterase or butyrylcholinesterase activity. Consequently, there is limited information from which a detailed understanding of structure-activity relationships can be derived. However, some halogenated derivatives are not only more potent acetylcholinesterase inhibitors than tacrine, they are also more selective for acetylcholinesterase than for butyrylcholinesterase.

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• Item metadata

  Item type:	Article
  ID code:	31615
  Dates:	Date Event 2000 Published
  Keywords:	acetylcholinesterase, aniline compounds, butyrylcholinesterase, cholinesterase inhibitors, cyanoketone, cyclohexanones, esters, nitriles, structure-activity relationship, tacrine, Pharmacy and materia medica, Molecular Medicine, Pharmacology
  Subjects:	Medicine > Pharmacy and materia medica
  Department:	Faculty of Science > Strathclyde Institute of Pharmacy and Biomedical Sciences
  Depositing user:	Pure Administrator
  Date deposited:	13 Jul 2011 08:56
  Last modified:	18 Jun 2021 02:52
  URI:	https://strathprints.strath.ac.uk/id/eprint/31615