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Enaminones-Versatile Therapeutic Pharmacophores. Further Advances

[ Vol. 7 , Issue. 4 ]

Author(s):

N. D. Eddington, D. S. Cox, R. R. Roberts, J. P. Stables, C. B. Powell and K. R. Scott   Pages 417 - 436 ( 20 )

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

Affiliation:

Department of Pharmaceutical Sciences, School of Pharmacy, Howard University, Washington, DC 20059 USA



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