Design, synthesis, and anticonvulsant activity of some sulfamides.
As part of our search for potential anticonvulsant agents, a set of compounds were designed, synthesized, and evaluated against MES and PTZ tests. Bioisosteric functional group information was used to design a new functionality, sulfamides, that complies with the requirements of the pharmacophore previously defined. Some of the molecules showed a promising anticonvulsant profile as selective anti-MES drugs, being active at low concentrations (30mg/kg). The biological data were confirmed in Phase II of the Anticonvulsant Drug Development Program of the National Institute of Health.
Gavernet
L
L
Medicinal Chemistry, Department of Biological Sciences, National University of La Plata, 47 and 115, La Plata B1900BJW, Argentina.
Barrios
I A
IA
Cravero
M Sella
MS
Bruno-Blanch
L E
LE
D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D004583:Electrons; D008297:Male; D051379:Mice; D008958:Models, Molecular; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013455:Sulfur / Q000737:chemistry*
D000577:Amides; D000927:Anticonvulsants; D013455:Sulfur