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Current Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Enaminones-Versatile Therapeutic Pharmacophores. Further Advances

Author(s): N. D. Eddington, D. S. Cox, R. R. Roberts, J. P. Stables, C. B. Powell and K. R. Scott

Volume 7, Issue 4, 2000

Page: [417 - 436] Pages: 20

DOI: 10.2174/0929867003375092

Price: $65

Abstract

Enaminones, enamines of ß-dicarbonyl compounds, have been know for many years. In our initial account (Current Med. Chem. 1994, 1, 159-175), we reported on the anticonvulsant activity of a series of enaminones, notably methyl 4-[(p-chlorophenyl)amino]-6-methyl- 2-oxo-cyclohex-3-en-1-oate, 9a (R=CH 3 , R 1 =4-Cl), which, in animal tests, compared favorably to phenytoin and carbamazepine. Since that time, further research in our laboratory and other laboratories have expanded the therapeutic potential of these compounds. In addition to new anticonvulsant derivatives, we have uncovered a novel brain transport mechanism for the enaminones and developed a preliminary regression model for further synthetic direction. These topics will each be presented and elaborated.

Keywords: enaminones versatile therapeutic pharmacophores, pyrrolidino enaminones, carbomethoxy, steric interactions, multisubstitution, carbomethoxy monochloro analogues, isoxazoles, tonic clonic seizures, spartan programs, congruent spatial relationship, bmec model, chromatographic retention


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