Novel phosphinic and phosphonic acid analogues of the anticonvulsant valproic acid.
1-Propylbutylphosphinic acid 2, (1-propylbutyl)methylphosphinic acid 3 and 1-propylbutylphosphonic acid 4 have been synthesized as bioisosteres of the corresponding carboxylic acid valproate 1, which is a potent anticonvulsant. The novel phosphinic and phosphonic acids were tested for their anticonvulsant activity and were found to be inactive.
Kehler
L
L
Department of Medicinal Chemistry, H. Lundbeck A/S, Valby, Denmark. jke@lundbeck.com
Hansen
H I
HI
Sanchez
C
C
D000818:Animals; D000927:Anticonvulsants / Q000737:chemistry* / Q000494:pharmacology; D063065:Organophosphonates / Q000737:chemistry*; D010721:Phosphinic Acids / Q000737:chemistry*; D051381:Rats; D014635:Valproic Acid / Q000031:analogs & derivatives* / Q000494:pharmacology
D000927:Anticonvulsants; D063065:Organophosphonates; D010721:Phosphinic Acids; D014635:Valproic Acid