Reference : Synthesis and pharmacological evaluation of a second generation of pyridothiadiazine ...
Scientific journals : Article
Human health sciences : Pharmacy, pharmacology & toxicology
Physical, chemical, mathematical & earth Sciences : Chemistry
http://hdl.handle.net/2268/5684
Synthesis and pharmacological evaluation of a second generation of pyridothiadiazine 1,1-dioxides acting as AMPA potentiators.
English
Francotte, Pierre mailto [Université de Liège - ULg > Département de pharmacie > Chimie pharmaceutique >]
De Tullio, Pascal mailto [Université de Liège - ULg > Département de pharmacie > Chimie pharmaceutique >]
Podona, Tchao [> > > >]
Diouf, Ousmane [> > > >]
Fraikin, Pierre mailto [Université de Liège - ULg > Département de pharmacie > Chimie pharmaceutique >]
Lestage, Pierre [Institut de Recherches Servier > > > > > >]
Danober, Laurence [Institut de Recherches Servier > > > > > >]
Thomas, Jean-Yves [Institut de Recherches Servier > > > > > >]
Caignard, Daniel-Henri [Institut de Recherches Servier > > > > > >]
Pirotte, Bernard mailto [Université de Liège - ULg > Département de pharmacie > Chimie pharmaceutique >]
2008
Bioorganic & Medicinal Chemistry
Elsevier Science
16
23
9948-56
Yes (verified by ORBi)
International
0968-0896
1464-3391
Oxford
United Kingdom
[en] Animals ; Diazoxide/chemistry/pharmacology ; Oocytes/drug effects/physiology ; Rats ; Rats, Wistar ; Receptors, AMPA/biosynthesis/drug effects/genetics ; Solubility ; Structure-Activity Relationship ; Thiadiazines/chemical synthesis/chemistry/pharmacology ; Xenopus laevis ; alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid/chemistry/pharmacology
[en] Taking into account structure-activity relationships obtained with our previous series, new diversely substituted 1,2,4-pyridothiadiazine 1,1-dioxides were designed to obtain novel AMPA potentiators. The aim of this work was focused on the improvement of lipophilicity, which is well known as a critical parameter to obtain in vivo active central nervous system agents. For this purpose, two positions on the pyridine ring were privileged to insert selected groups. Among the synthesized compounds emerged 7-chloro-4-ethyl-3,4-dihydro-2H-pyrido[2,3-e]-[1,2,4]-thiadiazine 1,1-dioxide (12d), which was evaluated in two memory tests in Wistar rats and showed cognition enhancing effects after intraperitoneal injection at doses as low as 0.3mg/kg.
http://hdl.handle.net/2268/5684
10.1016/j.bmc.2008.10.036

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