title: Design and development of 2,3-benzodiazepine (CFM) noncompetitive AMPA receptor antagonists.
abstract: 2,3-Benzodiazepines represent a class of heterocyclic compounds that interact with AMPA-type glutamate receptors in a noncompetitive manner. These compounds have attracted great interest for their pharmacological effects against acute and chronic neurodegenerative diseases, such as ischemia and epilepsy. We synthesized a large number of 2,3-benzodiazepine derivatives, which showed anticonvulsant properties in different seizure models and a noncompetitive blockade of AMPA receptor. This article will briefly mention our work in this field and the main SAR considerations.
authors.affiliation: Dipartimento Farmaco-Chimico, Università di Messina, Italy. gittoros@pharma.unime.it
authors.forename: Rosaria
authors.initials: R
authors.lastname: Gitto
authors.forename: Maria
authors.initials: M
authors.lastname: Zappal
authors.forename: Sarro Giovambattista
authors.initials: SG
authors.lastname: De
authors.forename: Alba
authors.initials: A
authors.lastname: Chimirri
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000627:therapeutic use; D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000627:therapeutic use; D001665:Binding Sites / Q000187:drug effects; D015195:Drug Design; D051379:Mice; D008811:Mice, Inbred DBA; D015394:Molecular Structure; D018091:Receptors, AMPA / Q000037:antagonists & inhibitors* / Q000378:metabolism; D012640:Seizures / Q000188:drug therapy; D013329:Structure-Activity Relationship
chemical_list: D000927:Anticonvulsants; D018091:Receptors, AMPA; D001569:Benzodiazepines