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Design, synthesis, and anticonvulsant activity of some sulfamides
- Source :
- Bioorganic & Medicinal Chemistry. 15:5604-5614
- Publication Year :
- 2007
- Publisher :
- Elsevier BV, 2007.
-
Abstract
- 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.
- Subjects :
- Male
Models, Molecular
medicine.medical_treatment
Clinical Biochemistry
Pharmaceutical Science
Electrons
Pharmacology
Biochemistry
Chemical synthesis
Mice
Structure-Activity Relationship
chemistry.chemical_compound
Drug Discovery
medicine
Animals
Molecular Biology
Molecular Structure
Chemistry
Organic Chemistry
Rational design
Biological activity
Amides
Anticonvulsant Agent
Anticonvulsant
Drug development
Drug Design
Molecular Medicine
Anticonvulsants
Bioisostere
Pharmacophore
Sulfur
Subjects
Details
- ISSN :
- 09680896
- Volume :
- 15
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....745e49c34cbc3f13800daa3d15c955b9
- Full Text :
- https://doi.org/10.1016/j.bmc.2007.05.024