|
Pazinaclone (DN-2327) is a sedative and anxiolytic drug in the cyclopyrrolone family of drugs. Other cyclopyrrolone drugs include zopiclone and eszopiclone. Pazinaclone has a very similar pharmacological profile to the benzodiazepine family of drugs including sedative and anxiolytic properties, but with less amnestic effects,〔Wada T, Fukuda N. Effect of a new anxiolytic, DN-2327, on learning and memory in rats. Pharmacology, Biochemistry and Behavior. 1992 Mar;41(3):573-9.〕 and at low doses it is a relatively selective anxiolytic, with sedative effects only appearing at higher doses.〔Suzuki M, Uchiumi M, Murasaki M. A comparative study of the psychological effects of DN-2327, a partial benzodiazepine agonist, and alprazolam. Psychopharmacology (Berlin). 1995 Oct;121(4):442-50.〕 Pazinaclone produces its sedative and anxiolytic effects by acting as a partial agonist at GABAA benzodiazepine receptors, although pazinaclone is more subtype-selective than most benzodiazepines.〔Atack JR. The benzodiazepine binding site of GABA(A) receptors as a target for the development of novel anxiolytics. Expert Opinion on Investigational Drugs. 2005 May;14(5):601-18.〕 ==Synthesis== Reaction of 2-Amino-7-chloro-1,8-naphthyridine with phthalic anhydride leads to the corresponding phthalimide. Selective reduction of one of the imide carbonyl groups in essence converts that to an aldehyde. Condensation with ''tert''-Butyl(triphenylphosphoranylidene)acetate gives the Wittig product. The carboxylic acid is then treated with Diethyl cyanophosphonate to convert that to an activated acid cyanide; reaction with 1,4-Dioxa-8-azaspiro(4.5)decane results in formation of the corresponding amide, pazinaclone. 抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』 ■ウィキペディアで「Pazinaclone」の詳細全文を読む スポンサード リンク
|