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ABSTRACT:
SUBMITTER: Goffin E
PROVIDER: S-EPMC6052356 | biostudies-literature | 2018 Jan
REPOSITORIES: biostudies-literature
Journal of medicinal chemistry 20171219 1
We report here the synthesis of 7-phenoxy-substituted 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides and their evaluation as AMPA receptor positive allosteric modulators (AMPApams). The impact of substitution on the phenoxy ring and on the nitrogen atom at the 4-position was examined. At GluA2(Q) expressed in HEK293 cells (calcium flux experiment), the most potent compound was 11m (4-cyclopropyl-7-(3-methoxyphenoxy)-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide, EC<sub>50</sub> = 2.0 nM) ...[more]