Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 15, Issue 16, Pages 5604-5614Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2007.05.024
Keywords
sulfamides; anticonvulsant; rational design; bioisosteres; pharmacophore
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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 (30 mg/kg). The biological data were confirmed in Phase II of the Anticonvulsant Drug Development Program of the National Institute of Health. (c) 2007 Elsevier Ltd. All rights reserved.
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