Synthesis and pharmacological evaluation of a second generation of pyridothiadiazine 1,1-dioxides acting as AMPA potentiators.

in Bioorganic & Medicinal Chemistry (2008), 16(23), 9948-56

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 ... [more ▼]

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. [less ▲]

Synthesis and pharmacological evaluation of ATP-sensitive potassium channel openers related to cromakalim: introduction of arylsulfonylurea or benzothiadiazinedioxide moieties

Poster (1998, September)

Synthesis and pharmacological evaluation of cromakalim analogues as potassium channel activators

Poster (2002, November 15)

Synthesis and pharmacological evaluation of novel thromboxane modulators as antiplatelet agents acting on both the alpha and beta isoforms of the human thromboxane receptor

in Journal of Medicinal Chemistry (2006), 49(12), 3701-3709

Synthesis and pharmacological evaluation of pyridinic methanesulfonamides as potential COX-2 inhibitors

Conference (2001, May)

Synthesis and pharmacological evaluation of pyridinic sulfonamides related to nimesulide

Poster (2001, November 16)

Synthesis and pharmacological evaluation of succinic acid receptor (SUCNR1) small molecule modulators

Poster (2012, November 30)

Synthesis and pharmacology of N"-(4-arylaminopyrid-3-yl)sulfonyl-N-cyano-N'-isopropylguanidines

Poster (1994, May)

Synthesis and pharmacology of pyrid-3-ylsulfonylcyanoguanidines as diuretics

in European Journal of Medicinal Chemistry (1995), 30

Synthesis and physico-chemical characterization of fatty esters

Poster (2012, November 16)

Specific antioxidant molecules (e.g. phenolics) help to prevent oxidation reaction of the cell membrane. A fatty chain grafted on these compounds should enhance their capacity to interact with the ... [more ▼]

Specific antioxidant molecules (e.g. phenolics) help to prevent oxidation reaction of the cell membrane. A fatty chain grafted on these compounds should enhance their capacity to interact with the membrane lipids. In our study, three fatty esters comprising an aromatic part were synthesized. They differentiate the aromatic substituent and the number of carbons between the aromatic ring and the ester function. A structure-function relationships study was performed to identify the structural pattern affecting the interfacial properties and the membrane interaction properties. The behavior of their monolayer film at an air-water interface was studied. The interactions with membrane were assessed on living cells and were predicted by a computational approach. In the future, we will investigate the effect of the presence of a sugar unit on these molecules. [less ▲]