Enaminones-Versatile Therapeutic Pharmacophores. Further Advances

Title: Enaminones-Versatile Therapeutic Pharmacophores. Further Advances

Volume: 7 Issue: 4

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

Affiliation:

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

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.

Cite this article as:

Eddington D. N., Cox S. D., Roberts R. R., Stables P. J., Powell B. C. and Scott R. K., Enaminones-Versatile Therapeutic Pharmacophores. Further Advances, Current Medicinal Chemistry 2000; 7 (4) . https://dx.doi.org/10.2174/0929867003375092