Synthesis and AMPA receptor antagonistic activity of a novel 7-imidazolyl-6-trifluoromethyl quinoxalinecarboxylic acid with a substituted phenyl group and improved its good physicochemical properties by introduced CF 3 group

Bioorganic and Medicinal Chemistry Letters

Volumn 14, Issue 20, 2004, Pages 5107-5111

  Takano, Yasuo ^a   Shiga, Futoshi ^a   Asano, Jun ^a   Hori, Wataru ^a   Anraku, Tsuyosi ^a   Uno, Takashi ^a  

^a KYORIN PHARMACEUTICAL CO LTD   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

7 IMIDAZOLYL 6 TRIFLUOROMETHYLQUINOXALINE CARBOXYLIC ACID; AMPA RECEPTOR ANTAGONIST; CARBOXYLIC ACID; UNCLASSIFIED DRUG;

AQUEOUS SOLUTION; ARTICLE; DRUG POTENCY; DRUG SELECTIVITY; DRUG SOLUBILITY; DRUG SYNTHESIS; PHYSICAL CHEMISTRY; SUBSTITUTION REACTION;

ANIMALS; BRAIN ISCHEMIA; DISEASE MODELS, ANIMAL; IMIDAZOLES; INFUSIONS, INTRAVENOUS; NEUROPROTECTIVE AGENTS; QUINOXALINES; RATS; RECEPTORS, AMPA; SOLUBILITY; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 4544326115     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2004.07.093     Document Type: Article

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21. Evaluation of the rat focal ischemia model: After 24 h of MCA occlusion as described by Tamura et al., brains were removed and sliced into five coronal (2-mm thick) sections with the use of a rat brain matrix (a manual slicer). Slices were placed in 2% (w/v) triphenyltetrazolium chloride (TTC) solution, and then in 10% (v/v) phosphate-buffered formalin. Tissue damage (areas not stained with TTC) was scored on a four-point scale (see figure A). Each test compound was administered by continuous iv infusion for 4 h, starting immediately after occlusion of the MCA. Control rats received saline only, and their four-point scale value was less than 1.0. As comparable compounds, NBQX was purchased from Sigma-Aldrich chemical Co., and YM-90K and YM-872 were obtained following the above reported procedures (YM-90K, Ref. 5; YM-872, Ref. a)
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