synthesis and Structure-Activity Relationships of 2,3-Benzodiazepines as AMPA Receptor Antagonists

Authors: Zappala M.; Grasso S.; Micale N.; Polimeni S.; De Micheli C.

Source: Mini Reviews in Medicinal Chemistry, Volume 1, Number 3, September 2001 , pp. 243-253(11)

Publisher: Bentham Science Publishers

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Abstract:

There is increasing evidence of the potential therapeutic utility of glutamate receptor antagonists in the treatment of several neurodegenerative disorders, including stroke and epilepsy. In the last few years noncompetitive AMPA receptor antagonists have received considerable attention due to their therapeutic potentiality. The discovery of GYKI 52466, the prototype of noncompetitive AMPA receptor antagonists endowed with anticonvulsant and neuroprotective properties, induced growing interest on 2,3-benzodiazepine derivatives. This review covers the chemistry and pharmacology of this important class of AMPA receptor antagonists.

Keywords: 2,3-Benzodiazepines; AMPA Receptor; glutamate receptor antagonists; neurodegenerative disorders; Stroke; Epilepsy; Anticonvulsant; Neuroprotective

Language: English

Document Type: Review article

DOI: http://dx.doi.org/10.2174/1389557013406783

Publication date: 2001-09-01

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The aim of Mini-Reviews in Medicinal Chemistry is to publish short reviews on the important recent developments in medicinal chemistry and allied disciplines.

The scope of Mini-Reviews in Medicinal Chemistry will cover all areas of medicinal chemistry including developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, drug targets, and natural product research and structure-activity relationship studies.

Mini-Reviews in Medicinal Chemistry is an essential journal for every medicinal and pharmaceutical chemist who wishes to be kept informed and up-to-date with the latest and most important developments.